ЗАМЕЩЕННЫЕ ДИГИДРО 3-ГАЛОГЕН-1H-ПИРАЗОЛ-5-КАРБОКСИЛАТЫ, ИХ ПОЛУЧЕНИЕ И ИСПОЛЬЗОВАНИЕ

Изобретение относится к новым соединениям формулы I и формулы II где R1 представляет собой галоген; R2 представляет галоген; R3 представляет C1-C4 алкил; Х представляет N или СН; и n равно 0-3, при условии, что когда Х представляет собой СН, тогда n равно, по меньшей мере, 1. где R1 представляет галоген; R2 представляет галоген; R3 представляет собой Н или C1-C4 алкил; Х представляет собой N или СН; и n равно от 0 до 3, при условии, что когда Х представляет собой СН, тогда n равно, по меньшей мере, 1. Изобретение также относится к способу получения соединения формулы I, способу получения соединения формулы II, способ получения соединения формулы III. Также описываются промежуточные соединения формулы 4. Технический результат - получение новых биологически активных соединений, которые представляют интерес в качестве инсектицидов, а также способ их получения. 6 н. и 18 з.п. ф-лы, 3 табл.

НОВЫЕ ПРОИЗВОДНЫЕ ГИДРОКСАМОВОЙ КИСЛОТЫ, ПОЛЕЗНЫЕ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ С ДЕГЕНЕРАЦИЕЙ СОЕДИНИТЕЛЬНОЙ ТКАНИ

Изобретение относится к производным гидроксамовой кислоты формулы I, где X означает -CH2-, -NR5-, -C(O); Y означает -CH2-, -NR5, при условии, что если X является -NR5-, то Y означает -CH2-; R1 означает H, C1-C20 алкил, -(CH2)j арил, -(CH2)j циклоалкил и др.; R2 означает H, C1-C20-алкил, -(CH2)j -R8, -(CH2)j -NR6R7, -(CH2)j -NR5-; -C(O)R5 и др.; R3 означает H, C1-C6алкил, -(CH2)j-арил, -(CH2)j - C3-6-циклоалкил и др., R5 означает H, C1-C6алкил, возможно замещенный 1 - 3 галогенами и др.; R6 и R7, одинаковые или различные, и означают H, C1-C6алкил и др., R8 означает -S-R8 и др., R9-галоген, C1 -C6 алкил и др., R10 - H; арил - фенил, возможно замещенный, Het - пиридинил, тиенил и др., i - 1 - 6, j - 0 - 4. Соединения I ингибируют избыток матрицы металлопротеиназы, что позволяет использовать их в фармацевтической композиции. 2 с. и 12 з.п.ф-лы, 1 табл.

СПОСОБ ПОЛУЧЕНИЯ 3-ГАЛОГЕН-4,5-ДИГИДРО-1Н-ПИРАЗОЛОВ

FIELD: chemistry. SUBSTANCE: invention refers to the method of preparation of 3-halogen-4.5-dihydro-1H-pyrasol compound of the formula , it includes interreaction with HX 1 of other 4.5-dihydro-1H-pyrasol compound of the formula , in which X 1 is halogen and R 3 , R 4 , Z, n and X 2 have values given in the description. The invention also describes preparation of the compounds of the formula , in which X 1 , R 3 , R 6 , R 7 , R 8a , R 8b and n have values, which are indicated in the description, in terms of the formula (Ia) of the compound, prepared according to p.1 of the invention formula. EFFECT: development of the alternative method of preparation of the compounds with using reagent of relatively low price. 9 cl, 1 tbl, 4 ex, 9 dwg ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 326 877 (13) C2 (51) ÌÏÊ C07D 401/04 C07D 231/06 C07D 231/14 (2006.01) (2006.01) (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2005105325/04, 29.07.2003 (72) Àâòîð(û): ÝÍÍÈÑ Ãàðè Äýâèä (US) (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 29.07.2003 (73) Ïàòåíòîîáëàäàòåëü(è): Å.È.ÄÞÏÎÍ ÄÅ ÍÅÌÓÐ ÝÍÄ ÊÎÌÏÀÍÈ (US) R U (30) Êîíâåíöèîííûé ïðèîðèòåò: 31.07.2002 (ïï.1-12) US 60/400,356 (43) Äàòà ïóáëèêàöèè çà âêè: 20.07.2005 (45) Îïóáëèêîâàíî: 20.06.2008 Áþë. ¹ 17 2 3 2 6 8 7 7 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: GB 1410191 À, 15.10.1973. WO 01/70671 A2, 27.09.2001, ñõåìû 10-17. RU 2137761 Ñ1, 20.09.1999. (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 28.02.2005 2 3 2 6 8 7 7 R U (87) Ïóáëèêàöè PCT: WO 2004/011453 (05.02.2004) C 2 C 2 (86) Çà âêà PCT: US 03/23820 (29.07.2003) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Å.Å.Íàçèíîé, ðåã. ¹ 517 (54) ÑÏÎÑÎÁ ÏÎËÓ×ÅÍÈß 3-ÃÀËÎÃÅÍ-4,5-ÄÈÃÈÄÐÎ-1Í-ÏÈÐÀÇÎËΠ(57) Ðåôåðàò: Äàííîå èçîáðåòåíèå îòíîñèòñ ê ñïîñîáó ïîëó÷åíè 3-ãàëîãåí-4,5-äèãèäðî-1Í-ïèðàçîëüíîãî ñîåäèíåíè ...

НОВЫЕ ПРОИЗВОДНЫЕ 4,5-ДИГИДРО-1H-ПИРАЗОЛА, ИМЕЮЩИЕ CB1-АНТАГОНИСТИЧЕСКУЮ АКТИВНОСТЬ

Настоящее изобретение относится к группе новых производных 4,5-дигидро-1Н-пиразола и их стереоизомерам и солям, которые являются сильными антагонистами рецептора каннабиноидов (CB1). Эти соединения пригодны для лечения ряда заболеваний, связанных с расстройствами каннабиноидной системы. Соединения имеют общую формулу (I), в которой R представляет собой фенил или тиенил, замещенный галогеном, или R представляет собой пиридил; R1 представляет собой фенил, который может быть замещен 1-2 заместителями, выбранными из галогена и трифторметила; R2 представляет собой водород; R3 представляет собой атом водорода или разветвленную или неразветвленную С1-4алкильную группу; R4 представляет собой разветвленную или неразветвленную С2-4алкильную группу, которая замещена гидрокси, амино, моноалкиламино, диалкиламино, метокси, ацетокси, аминоксигруппой или одним атомом фтора, или R4 представляет собой разветвленную или неразветвленную С1-8алкокси, которая может быть замещена аминогруппой, моноалкиламиногруппой ...

2-[(ДИГИДРО)ПИРАЗОЛИЛ-3'-ОКСИМЕТИЛЕН]АНИЛИДЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ, СРЕДСТВО БОРЬБЫ С СЕЛЬСКОХОЗЯЙСТВЕННЫМИ ВРЕДИТЕЛЯМИ И ВРЕДОНОСНЫМИ ГРИБАМИ И СПОСОБЫ БОРЬБЫ

Описываются новые соединения - 2-[(дигидро)пиразолил-3'-оксиметилен] анилиды формулы I, в которой означает простую, либо двойную связь, а индексы и заместители имеют следующее значение: n означает 0, 1 или 2; m означает 0, 1 или 2, причем заместители R2 могут быть различными, если m больше 1; Х означает прямую связь, О или NRa; Ra означает водород; R1 означает С1-С4алкил, галоген или в случае, когда n обозначает 2, представляет собой дополнительно связанный с двумя смежными атомами кольца углеводородный мостик, включающий 3 или 4 атома углерода; R2 означает нитро, галоген, С1-С4алкил, С1 -С4галогеналкил или С1-С4алкоксикарбонил; R3 означает необязательно замещенный алкил, необязательно замещенный насыщенный цикл, или необязательно замещенный одно-, либо двухъядерный ароматический радикал, который наряду с атомами углерода может содержать в качестве членов цикла от одного до четырех атомов азота; R4 означает водород, необязательно замещенный алкил; R5 означает алкил, или в случае, если Х ...

КОМБИНАТОРНЫЙ "SCAFFOLD" ПОДХОД К ФАРМАКОФОРАМ ЛИГАНДОВ РЕЦЕПТОРОВ УРОТЕНЗИНА II И СОМАТОСТАТИНА 5 ТИПА

... 1. Соединение формулы I или его соли где R1 и R3 независимо выбраны из группы, состоящей из водорода, необязательно замещенного карбонила(R), О(R), S(R), N(R)(R"), SO(R), SO2(R), алкила, алкенила, алкинила, циклоалкила, гетероциклила, арила и гетероарила, где указанные группы могут быть разветвленными или неразветвленными и могут быть необязательно замещены; R2 и R4-R6 независимо выбраны из группы, состоящей из водорода, необязательно замещенного О(R), S(R), N(R)(R"), алкила, алкенила, алкинила, циклоалкила, гетероциклила, арила и гетероарила, где указанные группы могут быть разветвленными или неразветвленными и могут быть необязательно замещены; R7 отсутствует или выбран из группы, состоящей из водорода, необязательно замещенного О(R), S(R), N(R)(R"), алкила, алкенила, алкинила, циклоалкила, гетероциклила, арила и гетероарила, где указанные группы могут быть разветвленными или неразветвленными и могут быть необязательно замещены; R8 выбран из группы, состоящей из водорода, необязательно ...

СИНТЕЗ ЗАМЕЩЕННЫХ ПРОИЗВОДНЫХ ПИРАЗОЛИН КАРБОКСАМИДИНА

... 1. Способ получения соединения формулы (I):или его таутомера, стереоизомера или фармакологически приемлемой соли, где:Rвыбран из водорода или (C)алкильной группы, необязательно замещенной одним-тремя атомами фтора или гидроксигруппой,Rпредставляет собой атом водорода или (C)алкильную группу, необязательно замещенную одним-тремя атомами фтора, гидроксигруппой, бензилоксиметильной группой, аминогруппой, монометиламиногруппой, диметиламиногруппой или Boc-, Fmoc- или Cbz-защищенной аминогруппой, где (C)алкильная группа может включать кетогруппу, сульфонильную группу или атом N, O или S,Rпредставляет собой атом водорода или (C)алкильную группу, необязательно замещенную одним-тремя атомами фтора, гидроксигруппой, бензилоксиметильной группой, аминогруппой, монометиламиногруппой, диметиламиногруппой или Boc-, Fmoc- или Cbz-защищенной аминогруппой, где (C)алкильная группа может включать кетогруппу, сульфонильную группу или атом N, O или S, илиRи Rсовместно с атомами углерода, отмеченными символами ...

Способ получения этилтиольных производных пиразола или пиразолина

Способ получения биспиразолинов N-нитраминодикетонов

Способ получения N-тиокар-бамил-3-(бета-окси-бета-метилпропил)-пиразолина

Способ получения 3-винилпиразолинов

COMPOSITION FOR PRODUCTION OF FLUORESCENT LIGHTING PIGMENT FOR POLYETHYLENE DYEING

4-[1-(4-SULFAMYLPHENYL)-5-PHENYL-2-PYRAZOLINYL-3]-1,8-NAPHTHOYLENE- 1',2'-BENZIMIDAZOLE AS A LUMINESCENT COMPOUND OF RED GLOW AND A LUMINESCENT COMPOSITION ON THE BASTS FOR POLYETHYLENE PAINTING

Способ получения 3-замещенных пиразолинов

Способ получения 3,5-дифенил-пиРАзОлА

Способ борьбы с насекомыми

СПОСОБ БОРЬБЫ С НАСЕКОМЫМИ путем обработки растений производным 1-фенш1карбамонп-3-

Способ получения арилоксипропаноламинов или их фармакологически приемлемых солей (его варианты)

... 1. Способ получения арилокси- пропаноламинов общей формулы I OCH CHCH NHXTSIHA in где R и Rj- одинаковые или различные и являются водородом низшей- алкокси-, циано-, окси- или бен- зилокси- группой; X - разветвленный или неразветвленный алкилен с 2-6 атомами углерода; А - тиофен, пиразолон, хи- ноксалин, хинолин, пиримидин , пурин, пирида- зин, пиримидин-2,4-ди- он, пиримидин-2-тион- 4-он, индазол, хиназолин , тетрагидроакридин, пиразол, пиридин, изо- хинолин, пиразоло ...

Способ получения пиразолиновых соединений

Способ получения сульфамидных производных альфа 2 -пиразолин-1-карбонамида

4,5-DIHYDROPYRAZOLVERBINDUNGEN, ARZNEIMITTEL UND IHRE VERWENDUNG

PYRAZOLINE, IHRE HERSTELLUNG UND IHRE VERWENDUNG ALS MITTEL MIT INSEKTIZIDER UND AKARIZIDER WIRKUNG

Substd. pyrazolines used as optical brighteners - esp. for synthetic polyamides and wool and prepn. from sulphochloride and thiosulphate derivs.

Optical brighteners for high mol. organic materials consist of new pyrazoline cpds. having general formula (I): (where M is H, alkali metal, NH4, mono- or di-alkylamine or mono- or di-(hydroxyalkyl)-amine; n is integer 1 to 5; X is H or COOH, Q is H or 1-4C alkyl; Y and Y1 is H, F or Cl; R1 and R2 each is H, D, Cl or 1-4C alkyl; R3 is H, F, Cl, 1-2C alkyl, or forms -C2H4- together with Z1; Z1 is H or 1-4C alkyl or forms -C2H4- together with R3 and Z2 is H, 1-4C alkyl or Ph opt. subst. by Cl, 1-3C alkyl or alkoxy, or Z1 and Z together form a gp. having formula (A), where U1 is H or CN, U2 is H, CN, COOH, opt. OH-substd. 2-5C carbaloxy or carbalmoyl or together with U3 forms a condensed benzene ring and U3 is H or 2-5C carbaloxy or together with U2 forms a condensed benzene ring). (I) are esp. used in wool and synthetic polyamides. Materials treated have a pure white blue-tinted fluorescent appearance.

VERFAHREN ZUR HERSTELLUNG VON PHENYLALKYLSULFONEN

INSEKTIZIDPRAEPARAT

PYRAZOLINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL FORMULATIONS CONTAINING THEM

CERTAIN 1-(3,5-DICHLOROBENZOYL)-3-PHENYLPYRAZOLINES AND THEIR USE AS MILDEWICIDES

VERWENDUNG VON PYRAZOLINDERIVATIVEN BEI DER HERSTELLUNG EINES MEDIKAMENTS ZUR PRÄVENTION UND/ODER BEHANDLUNG VON PROLIFERATIVEN ZELLERKRANKUNGEN

Aufhellungsmittel

Neue Pyrazolinderivate

NEW PYRAZOLINE DERIVATIVES

... 1286741 Optical brighteners. BADISCHE ANILIN & SODA FABRIK AG 2 Jan 1970 [4 Jan 1969] 208/70 Heading D1P [Also in Division C2] Optical brighteners for synthetic and natural polyamides, cellulose esters and acrylonitrile polymer textile materials comprise pyrazolines of the formula in which R is hydrogen, Cl, Br, methyl, methoxy, ethoxy, acetylamino, methyl sulphonylamino or acetoxy, R' is hydrogen, Cl, Br, methyl, ethyl, -COOH or ester or amide thereof, CN, SO 3 H or ester or amide thereof or sulphonyl, R2 is hydrogen, methyl or a carboxylic ester or amide, R3 is hydrogen or methyl, Y is hydrogen or Cl and X is hydroxy, alkoxy, aralkoxy, aryloxy, amino or substituted amino group. Specified substrates are wool, silk, nylon, cellulose acetate and triacetate. Example 86 describes the brightening of an acrylonitrile polymer cloth in an aqueous bath.

Pyrazoline Sulphonic Acid Esters

... 1,151,667. Pyrazoline sulphonic acid esters. J. R. GEIGY A.G. 22 Dec., 1967 [23 Dec., 1966], No. 58431/67. Heading C2C. [Also in Divisions C3, C5 and D1] Novel pyrazoline sulphonic acid esters of the general Formula (I) where R 1 is hydrogen, alkyl (C 1 -C 4 ), fluorine, chlorine, or bromine, Ar is a carbocyclic aromatic or heterocyclic aromatic radical unsubstituted or substituted by fluorine, chlorine, bromine, alkyl (C 1 -C 4 ), or alkoxy (C 1 -C 4 ), or arylamido groups, R 2 is hydrogen or alkyl (C 1 -C 4 ) or an alkylene group (C 1 -C 4 ) linked in the o-position with Ar, R 3 is hydrogen, alkyl (C 1 -C 4 ), or an aryl radical unsubstituted or substituted by fluorine, chlorine, bromine, alkyl (C 1 -C 4 ), alkoxy (C 1 -C 4 ) or by arylamido groups, and Z represents the aliphatic, araliphatic, or cyoloaliphatic radical of an alcohol or an aliphatic radical of an alcohol containing a heterocyclic ring system are prepared by reacting a sulphonic acid halide of the general formula where ...

DIPHENYL-PYRAZOLINES

... 1431104 Diphenylpyrazoline derivatives BASFAG 30 July 1973 [31 July 1972] 36118/73 Heading C2C Novel compounds of formula where A is unsubstituted or substituted alkyl or benzyl, R is C 1-4 alkyl or benzyl, R1 is H or unsubstituted or substituted alkyl or aralkyl, n is 0 or 1, X is H, Cl, Br, Me, Et, OMe or OEt and X- is an anion, R1 being other than H when n is 1, are prepared by reacting and quaternizing if desired. The products are optical brighteners. Methyl - 1 - (p - methylsulphonylphenyl) - 3- (p - chlorophenyl) - pyrazoline - #2 - 5 - carboxylate is prepared from p - chlorobenzaldehyde- - chloro - (p - methylsulphonyl) - phenylhydrazone and methyl acrylate.

Fluorescent 1-(Parazolinylphenylsulphonyl)-Piperazines

... 1,186,650. 1 - (Pyrayolinylphenylsalphonyl)- piperazines. J. R. GEIGY A.G. 11 Oct., 1968 [13 Oct., 1967], No. 48359/68. Heading C2C. [Also in Divisions C3, C5 and D1] Novel compounds of formula where Ar is a carbocyclic or heterocyclic aromatic radical optionally substituted by non- ionic, non-colour-imparting substituents; R 1 is optionally substituted alkyl, cycloalkyl, aralkyl, aryl or heterocyclic, or a modified, e.g. esterified, carboxyl group; R 2 , R 3 , R 4 and R 5 are independently H, F, Cl, Br, alkyl, cycloalkyl, aralkyl or aryl or R 2 and B 3 and/or R 4 and R 5 together represent alkylene which may be interrupted by arylene; R 6 is H, C 1-5 alkyl, F, Cl or Br; R 7 is H, C 1-5 alkyl, or aryl optionally substituted by non-ionic, non-colourimparting substituents; and R 8 is H, C 1-5 alkyl or a C 2-5 alkylene bridge to Ar in oposition to the pyrazoline ring, are prepared by reacting appropriate sulphonyl halides with appropriate piperazines. 1 (41 - Chlorosulphonylphenyl ...

MERCAPTOACYLDIHYDROPYRAZOLE CARBOXYLIC ACID DERIVATIVES

Methods for the synthesis of heteroaromatic compounds

PYRAZOLINE COMPOUNDS

... 1,209,631. Pyrazoline compounds. IMPERIAL CHEMICAL INDUSTRIES Ltd. 16 Feb.; 1968 [15 March, 1967], No. 12171/67. Heading C2C. [Also in Divisions C3 and D1] Novel pyrazoline compounds having the general formula wherein X represents a hydrogen atom, a halogen atom or an alkyl, alkoxy or acylamino group, Y represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, and Z represents an alkyl, alkenyl, substituted alkyl, aralkyl, aryl or substituted aryl group, are prepared by reacting a pyrazoline compound having the formula wherein X is as above and M represents an alkali metal atom or a trialkylammonium group, with an -halogenocarboxylic ester derivative having the formula wherein Hal represents a chlorine or bromine atom and Y and Z are as above, in the presence of a tertiary amine or an N,N-dialkyl-formamide, and optionally in the presence of a solvent, e.g. a hydrocarbon, a tertiary amine, or an excess of the -halogenocarboxylic ester, at 50-150‹ C.

4,5-DHYDRO 2 - LOWER - ALKOXYCARBONYLAMINO - 4 - PHENYLIMIDAZOLES AND SUBSTITUTED PHENYL DERIVATIVES THEREOF

CYANOPHENYL-PYRAZOLINES

Substituted pyrazolines

1-(4-CYANOPHENYL-CARBAMOYL)-PYRAZOLINE

Non-peptidyl inhibitors of vla-4 dependent cell binding useful in treating inflammatory autoimmune and respiratory diseases

Insecticidal 3-substitute 4-fluorophenyl-1-(fluoroalkoxyphenyl-carbomonyl)-pyrazolines.

Pyrazolines of ...

Pyrazoline insecticides

Pyrazoline Insecticides ...

Non-pepdyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases.

Compounds of Formula (1.0.0): are described wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably -C(=O)-; B is independently selected from a group of moieties, the most preferred of which are those of partial Formulas (1.1.2) and (1.1.6): and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial |y Formula (1.9.0):5 where R1a is hydrogen when R1 has the meaning of a mono-valent substituent; and R1a is a single bond when R1 has the meaning of a di-valent substituent. Said compounds are useful in methods of treating or preventing an inflammatory, autoimmune or respiratory diseases by inhibiting cell adhesion and consequent or associated pathogenic processes subsequently mediated by VLA-4.

Inhibitors of factor XA and other serine proteasesinvolved in the coagulation cascade

PYRAZOLINE INSECTICIDES

CYANOPHENYL-PYRAZOLINES

INSECTICIDAL 3-SUBSTITUTED 4-FLUOROPHENYL-1-(FLUORO-ALKOXYP HENYL-CARBAMOYL)-PYRAZOLINES

Non-peptidyl inhibitors of vla-4 dependent cell binding useful in treating inflammatory autoimmune and respiratory diseases

Substituted pyrazolines

Inhibitors of factor xa and other serine proteasesinvolved in the coagulation cascade.

Nitrosated and nitrosylated cyclooxygenase-2 inhibitors, compositions and methods of use

The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2(cox-2)inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2(cox-2)inhibitor, and optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous sythesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or optionally,at least ne therauptic agent, such as steroids, nonsteroidal antiinflamatory compounds (nsaid),5-lipoxygenase (5-lo)inhibitors, leukotriene b4 (ltb4)receptor antagonists, leukotriene a4 (lta4)hydrolase inhibitors, 5-ht agonists, 3 hydroxy-3-methylglutaryl coenzyme a (hmg-c0a)inhibitors,h2 antagonists, antineoplastic agents, antiplatelet agents, decongestants, diuretics, sedating or non-sedating or non-sedating anti-histamines, inducible nitric oxide sythase inhibitors, opioids, analsgesic, helicopter pylori inhibitors ...

Pyrazoline insecticides.

Composed of pyrazole, their preparation and their use.

Pyrazolines, their preparation and their application like insecticidal and acaricide products.

New pyrazoline compounds.

Pyrazoline insecticides.

Non-peptidyl inhibitors of VLA-4 dependent cell vinding useful in treating inflammatory, autoimmune,and respiratory diseases.

Derived from pyrazoline, their preparation and their application to the fight against insects and acarina.

Derived from pyrazoline.

Inhibitors of factor XA and other serine proteasesinvolved in the coagulation cascade.

Useful news pyrazoles like agents of regulation of the growth of plants

Inhibitors of factor xa and other serine proteasesinvolved in the coagulation cascade.

PYRAZOLINE INSECTICIDES

Nitrosated and nitrosylated cyclooxygenase-2 inhibitors compositions and methods of use

INSECTICIDAL 3-SUBSTITUTED 4-FLUOROPHENYL-1-(FLUORO-ALKOXYP HENYL-CARBAMOYL)-PYRAZOLINES

Inhibitors of factor xa and other serine proteasesinvolved in the coagulation cascade.

1-(4-CYANOPHENYL-CARBAMOYL)-PYRAZOLINE

Nitrosated and nitrosylated cyclooxygenase-2 inhibitors compositions and methods of use

PROCEDURE FOR THE PRODUCTION OF NEW ONE 1.3.4 - SUBSTITUTED PYRAZOLINDERIVATEN

INSECTICIDES ANTHRANILAMIDE

PYRAZOLIDINON CONNECTIONS AS LIGANDS OF THE EP2 AND/OR EP4 PRO DAY LAND IN RECEPTORS

VERFAHREN ZUR HERSTELLUNG VON NEUEN INDAZOLDERIVATEN UND IHREN SALZEN

HERBIZID

4,5-DIHYDRO (1H) - PYRAZOL DERIVATIVES AS CANNABINOID-CB1-REZEPTORMODULATOREN

VERFAHREN ZUR HERSTELLUNG VON NEUEN IMIDAZOLIN- DERIVATEN UND IHREN SALZEN

INSEKTIZIDE ZUSAMMENSETZUNGEN

VERFAHREN ZUR HERSTELLUNG VON ARYLSUBSTITUIERTEN PYRAZOLINEN UND VON DEREN SALZEN

TRANSFORMATION OF 2-PYRAZOLINEN INTO PYRAZOLE ASSISTANCE OF BROMIN

INSECTICIDE PREPARATION

INSECTICIDES COMPOSITIONS

INSECTICIDES ANTHRANILAMIDE

PROCEDURE FOR THE PRODUCTION OF NEW PYRAZOL-1 YL-PHENYLESSIGSAEUREN, THEIR SALTS AND OPTICAL ISOMERS

ANTI-IGNITING 4-AMINOPHENOL-DERIVATE.

INSECT-KILLING PYRAZOLINE.

GASTROKINETI AND ANTI- EMETI n (1SUBSTITUIERTE-4,5-DIHYDRO-1H-PYRAZOL-4YL) BENZAMIDE.

N-HETERO-CYCLIC ALCOHOL RENIN INHIBITORS.

PYRAZOLIN DERIVATIVES, PROCEDURES FOR THE PRODUCTION OF THESE CONNECTIONS AS WELL AS INSECTICIDES COMPOSITION ON THE BASIS OF THESE CONNECTIONS.

ON THERMAL WAY TRANSFERABLE ONE FLUORESCENT ONE DIPHENYLPYRAZOLINE.

1-CARBAMOYL-2-PYRAZOLIN-DERIVATE WITH HERBIZIDI EFFECT.

N-ARYL-3-ARYL-4,5-DIHYDRO-1H-PYRAZOL-1CARBOXAMIDE, PROCEDURE FOR THEIR PRODUCTION, IT CONTAINING INSECTICIDES COMPOSITIONS AND PROCEDURES FOR THE FIGHT AGAINST INSECTS.

VERFAHREN ZUR HERSTELLUNG VON NEUEN PHENYLCARBAMOYL-PYRAZOLINEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN 1,3,4- SUBSTITUIERTEN PYRAZOLINDERIVATEN

2-AMINOPROPANALACETALE, THEIR PRODUCTION, IT CONTAINING FUNGICIDES, THEIR PRODUCTION AND PROCEDURE FOR the FIGHT AGAINST MUSHROOMS.

Synthesis of substituted pyrazoline carboxamidine derivatives

This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.

Modulators of GTPase and Use In Relevant Treatment

The present invention relates to molecules which function as selective modulators of the Ras-homologous (Rho) family of small GTPases, in particular, Cdc42 GTPase and their use to treat diseases, for example cancers, including metastatic cancer, genetic and acquired diseases where activation of Cdc42 GTPase plays a pivotal role, such as neurodegenerative diseases, rheumatoid arthritis, atherosclerosis, diabetes type I, autosomal polycystic kidney disease, cystic kidney disease, precystic kidney disease, microbial infections, including infections, infections, infections and its secondary effects including gastric ulcers, (Q-fever) infections and infections, fungal infections including and and their secondary effects including lung edema. Additionally, compounds according to the present invention may be used to inhibit rejection in transplant patients (pursuant to transplantation), to promote immunosuppression, anti-inflammatory response and to mobilize stem cell (migration) in patients in need, among others. 1. (canceled)2. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)12. (canceled)13. A method of modulating Cdc42 GTPase in a patient or subject in need comprising administering to said patient or subject an effective amount of a compound according to .14. The method according to wherein said compound inhibitors Cdc42GTPase.15. A method of treating a disease state or condition in a patient or subject where modulation of GTPase provides a therapeutic advantage claim 3 , said method comprising administering to a patient or subject in need a compound according to to said patient or subject.16. The method according to wherein GTPase is overexpressed in tissues of said patient or subject and said modulation is inhibition of said GTPase.17. A method of inhibiting or treating cancer in a patient or subject in need comprising administering to said patient or subject an effective amount of a compound set forth in to said ...

ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS

This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in parkinson's disease, huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description. 119-. (canceled)27. The method of claim 22 , wherein the compound is an optically active enantiomer.28. The method of claim 22 , further comprising at least one additional therapeutic agent. This invention relates to the fields of pharmaceutical and organic chemistry, and provides arylsulfonyl pyrazoline carboxamidine derivatives, intermediates, formulations and methods.Serotonin (5-hydroxytryptamine or 5-HT), a key transmitter of the peripheral and central nervous system, modulates a wide range of physiological and pathological functions, mediated through a number of receptor families termed 5-HT, 5-HT, 5-HT, 5-HT, 5-HT, 5-HTand 5-HT. Although the functions of the latter three are less well understood than those of the others, it is generally accepted that compounds which selectively interfere with 5-HT-mediated signal transduction are ...

CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING DISEASE CONDITIONS, INCLUDING METABOLIC DISORDERS AND CANCERS

The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers. 2. A compound of claim 1 , wherein the compound is Example 1 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.3. A compound of claim 2 , wherein the stereomeric purity is at least 95%.4. A compound of claim 1 , wherein the compound is Example 2 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.5. A compound of claim 4 , wherein the stereomeric purity is at least 95%.6. A compound of claim 1 , wherein the compound is Example 3 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.7. A compound of claim 6 , wherein the stereomeric purity is at least 95%.8. A compound of claim 1 , wherein the compound is Example 4 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.9. A compound of claim 7 , wherein the stereomeric purity is at least 95%.10. A pharmaceutical composition claim 1 , comprising: a therapeutically effective amount of a compound of and a pharmaceutically acceptable carrier.11. A method of treating a disease claim 1 , comprising: administering to a mammal in need thereof a therapeutically effective amount of a compound of claim 1 , wherein the disease is selected from obesity claim 1 , diabetes claim 1 , dyslipidemias claim 1 , cardiovascular disorders claim 1 , inflammatory disorders claim 1 , hepatic disorders claim 1 , cancers claim 1 , and a combination thereof.12. The method of claim 11 , wherein the diabetes disorder is selected from Type 1 diabetes claim 11 , Type 2 diabetes claim 11 , inadequate glucose tolerance claim 11 , and insulin resistance.13. ...

Continuous production and reaction of a diazo compound

A process for producing a reaction product of a diazo compound, which process comprises: a. continuously supplying to a first reactor a precursor of a diazo compound; a water-miscible solvent; a base and water; b. mixing the precursor of a diazo compound; the water-miscible solvent; the base and water to generate a diazo compound; c. continuously removing from the first reactor, through a hydrophobic membrane, into a second reactor the formed diazo compound; d. continuously removing from the first reactor all reaction products that have not passed into the second reactor; e. continuously supplying to the second reactor a substrate in a non-water-miscible solvent; f. mixing the above components to generate a reaction product of a diazo compound; and g. continuously removing from the second reactor the non-water-miscible solvent and the reaction product of the diazo compound, and apparatus suitable for carrying out such a process.

BROMOPHENOL-PYRAZOLINE COMPOUND AND SYNTHESIS METHOD AND USE THEREOF

The present invention relates to a compound, and in particular to a bromophenol-pyrazoline compound and a synthesis method and use thereof. The bromophenol-pyrazoline compound is represented by a general structural formula below: 6. Use of a bromophenol-pyrazoline compound according to in inhibiting the replication of coronavirus.7. Use of a bromophenol-pyrazoline compound according to in inhibiting the replication of coronavirus.8. Use of a bromophenol-pyrazoline compound according to in the preparation of drugs for treating coronavirus pneumonia.9. A drug for treating coronavirus pneumonia claim 1 , comprising an effective dose of one or a mixture of two or more of the a bromophenol-pyrazoline compounds according to .10. A drug for treating coronavirus pneumonia claim 2 , comprising an effective dose of a bromophenol-pyrazoline compound according to claim 2 , or a mixture of two or more thereof. The present invention relates to a compound, and particularly to a bromophenol-pyrazoline compound and a synthesis method and use thereof.The new coronavirus is an enveloped positive-sense type B single-stranded RNA coronavirus. During the life cycle of the coronavirus, all replications and transcriptions are performed by the polyprotein replicases ppla and pplab. Before becoming a mature functional protein, ppla and ppab need to be hydrolyzed in the presence of the host's cellular enzyme, and they are active only after hydrolysis. This important polyproteolytic process in the life cycle of the virus is completed by the main protease (M) encoded by the virus, and is essential for processing polyproteins translated from viral RNA. Therefore, inhibiting the activity of this enzyme can effectively suppress viral replicationCountries around the world are speeding up the development of novel coronavirus pneumonia vaccines, and some vaccines have entered the clinical trial stage. However, there are multiple serotypes of coronaviruses, which can produce repeated infections; and ...

CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING DISEASE CONDITIONS, INCLUDING METABOLIC DISORDERS AND CANCERS

The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers. 2. The method of claim 1 , wherein the compound is compound 1 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.3. The method of claim 2 , wherein the stereomeric purity is at least 95%.4. The method of claim 1 , wherein the compound is compound 2 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.5. The method of claim 4 , wherein the stereomeric purity is at least 95%.6. The method of claim 1 , wherein the compound is compound 3 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.7. The method of claim 6 , wherein the stereomeric purity is at least 95%.8. The method of claim 1 , wherein the compound is compound 4 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.9. The method of claim 8 , wherein the stereomeric purity is at least 95%.1019-. (canceled)20. The method of claim 1 , wherein the co-morbidity of obesity is selected from diabetes claim 1 , dyslipidemias claim 1 , Metabolic Syndrome claim 1 , dementia claim 1 , cardiovascular disease claim 1 , hepatic disease claim 1 , hypertension claim 1 , gallbladder disease claim 1 , gastrointestinal disorders claim 1 , menstrual irregularities claim 1 , degenerative arthritis claim 1 , venous stasis ulcers claim 1 , pulmonary hypoventilation syndrome claim 1 , sleep apnea claim 1 , snoring claim 1 , coronary artery disease claim 1 , arterial sclerotic disease claim 1 , pseudotumor cerebri claim 1 , accident proneness claim 1 , increased risks with surgeries claim 1 , osteoarthritis claim 1 , high cholesterol claim 1 ...

CANNABINOID RECEPTOR MEDIATING COMPOUNDS

A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CBreceptor mediating scaffold conjugated to (ii) a second therapeutic scaffold. 3. The compound of claim 2 , wherein Ris H claim 2 , hydroxy claim 2 , C-Calkyl claim 2 , or acyl.4. The compound of claim 2 , wherein Ris C-Calkyl claim 2 , C-Ccycloalkyl claim 2 , amino claim 2 , phenyl claim 2 , heteroaryl claim 2 , acyl or heterocycloalkyl.5. The compound of claim 2 , wherein Ris H.78-. (canceled)10. (canceled)11. The compound of claim 1 , wherein a and c are each one claim 1 , Ris halogen claim 1 , and Ris halogen.12. The compound of claim 1 , wherein b is zero.13. The compound of claim 1 , wherein X is SO.16. The compound of claim 15 , wherein A is —NH—NH.18. The compound of claim 17 , wherein Ris methyl claim 17 , phenyl claim 17 , —NHBoc claim 17 , pyridinyl claim 17 , cyclopropyl claim 17 , tert-butyl claim 17 , morpholinyl claim 17 , pyrrolidinyl claim 17 , or —N(methyl).20. The compound of claim 19 , wherein Ris H claim 19 , acyl claim 19 , or C-Calkyl.23. (canceled)25. The compound of claim 1 , wherein A constitutes at least a portion of a therapeutic scaffold.26. The compound of claim 25 , wherein the therapeutic scaffold comprises an antidiabetic agent claim 25 , an anticancer agent claim 25 , or an antiobesity agent.27. (canceled)28. A compound claim 25 , or a pharmaceutically acceptable salt or ester thereof claim 25 , comprising (i) a CBreceptor mediating scaffold and (ii) a second therapeutic scaffold.29. The compound of claim 28 , wherein the second therapeutic scaffold comprises an antidiabetic agent claim 28 , an anticancer agent claim 28 , or an antiobesity agent.30. The compound of claim 28 , wherein the compound is a 3-phenyl-N′-phenyl-N-imino-1H-pyrazole-1-carboximidiamide compound.31. The compound of claim 28 , wherein the CBreceptor mediating scaffold comprises a 3-phenyl-N′-phenyl-1H-pyrazole-1-carboximidiamide scaffold.32. The compound of claim 1 , wherein ...

ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS

This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description. 18-. (canceled)16. The method of claim 11 , wherein the compound is an optically active enantiomer.17. The method of claim 11 , further comprising at least one additional therapeutic agent. This invention relates to the fields of pharmaceutical and organic chemistry, and provides arylsulfonyl pyrazoline carboxamidine derivatives, intermediates, formulations and methods.Serotonin (5-hydroxytryptamine or 5-HT), a key transmitter of the peripheral and central nervous system, modulates a wide range of physiological and pathological functions, mediated through a number of receptor families termed 5-HT, 5-HT, 5-HT, 5-HT, 5-HT, 5-HTand 5-HT. Although the functions of the latter three are less well understood than those of the others, it is generally accepted that compounds which selectively interfere with 5-HT-mediated signal transduction are ...

Aromatic compounds with sulfur containing ligands

Compounds useful as nutritional supplements, antioxidants, heavy metal chelators and/or as intermediates for producing other related compounds with like uses have a formula: where R 1 is an aromatic backbone and R 2 is a sulfur containing ligand.

PROCESS FOR PRODUCING ISOXAZOLINE DERIVATIVES

A process for producing isoxazoline derivatives by ring-opening and cyclization of the corresponding cyclopropane derivatives with electrophilic nitrosylation reagents. 2. A process according to wherein both Arand Arare phenyl groups claim 1 , and R is ethoxycarbonyl group.3. A process according to wherein the cyclpropane derivative is ethyl 2 claim 1 ,2-diphenylcyclopropanylcarboxylate.4. A process according to wherein the electrophilic nitrosylation regent is at least one member selected from the group consisting of nitrosylchloride claim 1 , nitrosylbromide claim 1 , nitrosylsulfonic acid claim 1 , and electrophilic nitrosylation reagents comprising at least one member of nitrite salts selected from the group consisting of lithium nitrite claim 1 , sodium nitrite claim 1 , potassium nitrite and one member of strong acid selected from the group consisting of hydrogen chloride claim 1 , hydrogen bromide claim 1 , sulphuric acid claim 1 , nitric acid claim 1 , trifluoroacetic acid claim 1 , boron trifluoride claim 1 , boron trichloride claim 1 , aluminium chloride.5. A process according to wherein the nitrosylation reagent is composed of sodium nitrite and sulphuric acid; the sulphuric acid is used in an amount of 3.0 moles to 30.0 moles per mole of sodium nitrite.6. A process according to wherein the cyclpropane derivative is used at a concentration of 0.1 moles per litre to 10.0 moles per litre.7. A process according to wherein the nitrosylation reagent is used in an amount of 1.0 mole to 10.0 moles for every one mole of the cyclopropane derivative used.8. A process according to wherein the nitrosylation reagent is used in an amount of approximately 1.1 moles per mole of the cyclopropane derivative.9. A process according to further comprises a solvent wherein the solvent is at least one member selected from hydrocarbons claim 1 , chlorinated hydrocarbons claim 1 , aromatic hydrocarbons claim 1 , esters claim 1 , ethers claim 1 , halogenated aromatic hydrocarbons ...

USE OF PHENYLPYRAZOLIN-3-CARBOXYLATES FOR IMPROVING PLANT YIELD

Compounds (A) can be used for increasing the yield of useful plants or crop plants with respect to their harvested plant organs, wherein the Compound (A) is selected from compounds of the formula (I) or salts thereof, 2. The method according to claim 1 , wherein{'sup': 1', '1', '1, 'sub': n', '3, '(R)is n radicals Rwhere the Rare identical or different and are each F, Cl, Br or CF.'}n is 2 or 3.{'sup': '2', 'sub': 1', '4, 'Ris hydrogen or (C-C)-alkyl.'}{'sup': '3', 'sub': 1', '4', '2', '4', '2', '4, 'Ris hydrogen, (C-C)-alkyl, (C-C)-alkenyl or (C-C)-alkynyl.'}{'sup': '4', 'sub': 1', '8, 'Ris hydrogen or (C-C)-alkyl.'}3. The method according to claim 1 , wherein compound (A) is mefenpyr-diethyl.4. The method according to claim 1 , wherein Compound (A) is applied in combination with one or more compounds selected from the group of fungicides claim 1 , insecticides and plant growth regulators.5. The method according to claim 1 , comprising increasing the grain yield of crop plants selected from group consisting of cereals claim 1 , canola claim 1 , soybean and cotton crops.6. The method according to claim 1 , comprising increasing the grain yield of crop plants selected from group consisting of wheat claim 1 , barley claim 1 , rye or triticale plants. The method according to claim 1 , comprising increasing the gluten content of seed kernels of crop plants selected from group consisting of cereals claim 1 , canola and soybean crops.8. The method according to claim 1 , comprising increasing the gluten content of seed kernels of crop plants selected from group consisting of cereal crops.9. The method according to claim 1 , comprising increasing the protein content of seed kernels of crop plants selected from group consisting of cereals claim 1 , canola and soybean crops.10. The method according to claim 1 , comprising increasing the yield of the amount by weight of beets of beet plants.11. The method according to claim 1 , comprising increasing the sugar content of sugar ...

DERIVATIVES OF CELEBOXIB, USE THEREOF AND PREPARATION THEREOF

Derivatives of celecoxib that lack cyclooxygenase inhibitory activity but have improved PDE5 inhibitory activity are provided along with pharmaceutical compositions containing them for the treatment or prevention of cancer. Such compounds are expected to have reduced toxicity compared with celecoxib and other cyclooxygenase inhibitors, and greater efficacy compared with conventional PDE5 inhibitors. Derivatives of celecoxib are also suitable for treating chronic inflammatory conditions, erectile dysfunction, pulmonary hypertension, congestive heart failure, and enhancement of cognitive function. 2. A pharmaceutical composition comprising a compound of claim 1 , a pharmaceutically acceptable salt thereof claim 1 , a prodrug thereof claim 1 , a solvate thereof or a mixture thereof and a pharmaceutically acceptable carrier.3. A method of treating cancer in a mammal which comprises administering to the mammal an effective treatment amount of a compound of claim 1 , a pharmaceutically acceptable salt thereof claim 1 , a prodrug thereof claim 1 , a solvate thereof or mixture thereof.4. A method of treating a chronic inflammatory condition with reduced toxicity in a mammal which comprises administering to the mammal an effective treatment amount of a compound of claim 1 , a pharmaceutically acceptable salt thereof claim 1 , a prodrug thereof claim 1 , a solvate thereof or mixture thereof.5. A method of treating erectile dysfunction in a mammal which comprises administering to the mammal an effective treatment amount of a compound of claim 1 , a pharmaceutically acceptable salt thereof claim 1 , a prodrug thereof claim 1 , a solvate thereof or mixture thereof.6. A method for enhancing cognitive functions in a mammal which comprises administering to the mammal an effective treatment amount of a compound of claim 1 , a pharmaceutically acceptable salt thereof claim 1 , a prodrug thereof claim 1 , a solvate thereof or mixture thereof.7. A method of treating benign prostatic ...

Novel aryl-cyanoguanidine compounds

The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine- pyrazolines of general formula (I), wherein R 1 , R 2 , R 3 , R 4 and R 5 have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyperproliferative disorders, in particular for cancer, respectively tumour disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility.

Novel aryl-cyanoguanidine compounds

The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine-pyrazolines of general formula (I), wherein R 1 , R 3 , R 4 , R 5 and n have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyperproliferative disorders, in particular for cancer, respectively tumour disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility.

COMPOSITIONS AND METHODS FOR TREATMENT OF PAIN

The present disclosure relates to compositions comprising a transient receptor potential vanilloid-1 (TRPV1) antagonist and an alpha-2 adrenoreceptor agonist useful in the treatment of various forms of pain, including chronic pain (CP) syndromes, inflammatory pain and pain associated with neuropathy and other diseases and disease states; and methods of use thereof. 2. The pharmaceutical composition of claim 1 , wherein the compound of Formula (I) is selected from the group consisting of clonidine claim 1 , lofexidine claim 1 , guanfacine claim 1 , dexmedetomidine claim 1 , guanabenz claim 1 , tizanidine claim 1 , brimonidine claim 1 , xylazine and xylometazoline claim 1 , an enantiomer thereof claim 1 , a metabolite thereof claim 1 , a derivative thereof claim 1 , a prodrug thereof claim 1 , a pharmaceutically acceptable salt thereof claim 1 , or an acid addition salt or a combination thereof.3. The pharmaceutical composition of claim 1 , wherein the compound of Formula (II) is selected from the group consisting of N-(4-((6-(4-(trifluoromethyl)phenyl)pyrimidin-4-yl)oxy)benzo[d]thiazol-2-yl)acetamide claim 1 , 5′-chloro-1′-(3-fluorobenzyl)-7′-methylspiro[imidazolidine-4 claim 1 ,3′-indoline]-2 claim 1 ,2′ claim 1 ,5-trione claim 1 , (R)-1-(5-(tert-butyl)-2 claim 1 ,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea claim 1 , (S)-3-(hydroxymethyl)-4-(5-methylpyridin-2-yl)-N-(4-(2 claim 1 ,2 claim 1 ,2-trifluoroethoxy)phenyl)-3 claim 1 ,4-dihydro-2H-benzo[b][1 claim 1 ,4]oxazine-8-carboxamide claim 1 , (R)-1-(6-fluorospiro[chromane-2 claim 1 ,1′-cyclobutan]-4-yl)-3-(isoquinolin-5-yl)urea claim 1 , and N-(4-(trifluoromethyl)phenyl)-7-(3-(trifluoromethyl)pyridin-2-yl)quinazolin-4-amine; or an enantiomer thereof claim 1 , a metabolite thereof claim 1 , a derivative thereof claim 1 , a prodrug thereof claim 1 , a pharmaceutically acceptable salt thereof claim 1 , or an acid addition salt or a combination thereof.4. A method of treating pain comprising administering a TRPV1 ...

Novel form of mefenpyr-diethyl, a process for its preparation and use of the same

A crystalline form of mefenpyr-diethyl of formula (I), the crystal preparation process, the analyses of the crystal through various analytical methods and using the crystal to prepare stable agrochemical formulation. The invention also describes the use of various solvents towards the crystalline form preparation conditions.

FUNGICIDAL ACTIVE COMPOUND COMBINATIONS

Safeners for herbicides are suitable for increasing the microbicidal activity of fungicides. 1. A method of increasing the microbiocidal activity of a fungicide comprising treating a seed or a plant with the fungicide and a safener , wherein the safener is mefenpyr-diethyl and wherein the fungicide is fluoxastrobin , trifloxystrobin , or spiroxamine , wherein the mefenpyr and the fungicide are applied to the seed or plant in synergistic amounts , wherein the weight ratio of mefenpyr to fungicide is from 50:1 to 1:50.2. The method according to wherein the seed or the plant is treated with a composition comprising the fungicide and the safener.3. The method according to wherein the seed is treated with the fungicide and the safener.4. The method according to wherein the plant is treated with the fungicide and the safener.5. The method according to wherein the seed is in contact with the fungicide and the safener.6. The method according to wherein the plant is in contact with the fungicide and the safener.7. The method according to wherein the plant is a transgenic plant.8. The method according to claim 1 , wherein the weight ratio of mefenpyr-diethyl to the fungicide 10:1 to 1:20.9. The method according to claim 1 , wherein the fungicide is fluoxastrobin.10. The method according to claim 1 , wherein the fungicide is trifloxystrobin.11. The method according to claim 1 , wherein the fungicide is spiroxamine.12. A method of controlling phytopathogenic fungi comprising treating a seed or a plant with mefenpyr-diethyl and a fungicide selected from fluoxastrobin claim 1 , trifloxystrobin claim 1 , or spiroxamine claim 1 , wherein the mefenpyr and the fungicide are applied to the seed or plant in a weight ratio from 50:1 to 1:50.13. The method according to claim 12 , wherein the fungi is plasmodiophoromycetes claim 12 , oomycetes claim 12 , chytridiomycetes claim 12 , zygomycetes claim 12 , ascomycetes claim 12 , basidiomycetes claim 12 , or deuteromycetes.14Erysiphe ...

PYRAZOLE DERIVATIVES AND THEIR USE AS CANNABINOID RECEPTOR MEDIATORS

A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: 2. The compound of claim 1 , wherein Rand Rtogether with Z do not form an optionally-substituted cycloalkyl ring or an optionally-substituted heterocycloalkyl ring.3. The compound of claim 2 , wherein Rand Rare each independently optionally-substituted alkyl.4. The compound of claim 3 , wherein Rand Rare each the same and are each lower alkyl claim 3 , and Z is N.6. The compound of claim 1 , wherein each of X and Y is an optionally-substituted aryl.14. The compound of claim 13 , wherein Rand Rtogether with Z do not form an optionally-substituted cycloalkyl ring claim 13 , an optionally-substituted heterocycloalkyl ring; an optionally-substituted aryl ring claim 13 , or an optionally-substituted heteroaryl ring.15. The compound of claim 13 , Rand Rare each independently optionally-substituted alkyl (particularly lower alkyl).16. The compound of claim 15 , wherein Rand Rare each the same and are each lower alkyl claim 15 , and Z is N.24. The compound of claim 1 , wherein Ris optionally-substituted alkyl (e.g. claim 1 , lower alkyl claim 1 , thiol-substituted lower alkyl) claim 1 , aminocarbonyl (e.g. claim 1 , acetamido) claim 1 , or optionally-substituted phenyl (e.g. claim 1 , halogen-substituted phenyl).25. The compound of claim 1 , wherein Q is H.26. The compound of claim 1 , wherein A is —CH— claim 1 , —CF— claim 1 , —O— claim 1 , or —CH(CF)—.27. The compound of claim 1 , wherein D is —S(O)—.28. The compound of claim 1 , wherein n is 0.29. The compound of claim 1 , wherein X and Y are each optionally-substituted phenyl claim 1 , and Q is H.30. The compound of claim 1 , wherein the —NH—C(NH)R— moiety or —N═C(NH)R— moiety comprises a therapeutic scaffold selected from an antidiabetic agent claim 1 , an anticancer agent claim 1 , an antiobesity agent claim 1 , and an antifibrotic agent.31. The compound of claim 1 , wherein the —NH—C(NH)R— moiety or —N═C(NH)R— moiety comprises ...

CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING METABOLIC DISORDERS, INCLUDING OBESITY AND DIABETES

The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers. 2. The compound of claim 1 , wherein the stereomeric purity is at least 60%.3. The compound of claim 12 , wherein the stereomeric purity is at least 95%.4. canceled5. canceled6. canceled7. canceled8. canceled9. canceled10. A pharmaceutical composition claim 1 , comprising: a therapeutically effective amount a compound of and a pharmaceutically acceptable carrier.11. A method of treating a disease claim 1 , comprising: administering to a mammal in need thereof a therapeutically effective amount of a compound of one of - claim 1 , wherein the disease is selected from obesity claim 1 , diabetes claim 1 , dyslipidemias claim 1 , cardiovascular disorders claim 1 , inflammatory disorders claim 1 , hepatic disorders claim 1 , cancers claim 1 , and a combination thereof.12. The method of claim 11 , wherein the diabetes disorder is selected from Type 1 diabetes claim 11 , Type 2 diabetes claim 11 , inadequate glucose tolerance claim 11 , and insulin resistance.13. The method of claim 11 , wherein the dyslipidemia disorder is selected from undesirable blood lipid levels claim 11 , including low levels of high-density lipoprotein claim 11 , high levels of low-density lipoprotein claim 11 , high levels of triglycerides claim 11 , and a combination thereof.14. The method of claim 11 , wherein the cardiovascular disorder is selected from atherosclerosis claim 11 , hypertension claim 11 , stroke and heart attack.15. The method of claim 11 , wherein the inflammatory disorder is selected from osteoarthritis claim 11 , rheumatoid arthritis claim 11 , inflammatory bowel diseases claim 11 , and obesity-associated inflammation.16. The method of claim 11 , wherein the hepatic disorder is ...

MODULATORS OF GTPASES AND THEIR USE

The present invention relates to molecules which function as modulators (i.e., inhibitors and agonists) of the Ras-homologous (Rho) family of small GTPases (e.g. Rac, Cdc42 and Rho GTPases) and their use to treat diseases, including cancers (including solid tumors-medulloblastoma, ovarian, breast, head and neck, testicular, prostate among others and hematologic malignancies-B cell lymphoma, where these GTPases are overexpressed or hyperactivated), sporadic and genetic diseases where activation of Rho GTPases plays a pivotal role (Menkes disease, rheumatoid arthritis, atherosclerosis, diabetes (type 1), Huntington's disease and Alzheimer's disease) which are mediated through these proteins. Compounds according to the present invention may also be used as a therapy for the treatment of spp. or spp. infections, especially including 1. (canceled)2. A method to treat cancer in a patient comprising administering to a subject in need thereof an anti-cancer effective amount of a composition comprising R-ketorolac or a pharmaceutically acceptable salt thereof in combination with an angiogenesis inhibitor and a pharmaceutically acceptable carrier , additive or excipient , so as to treat said cancer patient.3. The method of claim 2 , wherein the R-ketorolac is enantiomerically pure.4. The method of claim 2 , wherein the angiogenesis inhibitor is bevacizumab claim 2 , everolimus claim 2 , lenalidomide claim 2 , lenvatinib mesylate claim 2 , pazopanib claim 2 , sorafenib claim 2 , sunitinib claim 2 , thalidomide or vandetanib.5. The method of claim 2 , wherein the cancer is selected from the group consisting of a carcinoma claim 2 , cancer of the esophagus claim 2 , head claim 2 , kidney claim 2 , liver claim 2 , lung claim 2 , nasopharyngeal claim 2 , neck claim 2 , ovary claim 2 , pancreas claim 2 , prostate claim 2 , and stomach claim 2 , a leukemia claim 2 , a malignant lymphoma claim 2 , a malignant melanoma claim 2 , a myeloproliferative disease claim 2 , a sarcoma claim 2 ...

PROCESS FOR MANUFACTURING 1-CYCLOPROPYL-NAPHTHALENES

A process for preparing 1-cyclopropyl-naphthalene derivatives of Formula (1) wherein R-Rare independently hydrogen, alkyl, alkoxy, cycloalkyl or aryl comprising the steps of a) contacting an acid salt of a 1-naphthyl-2-aminoethylketone with a base and a first solvent to obtain a solution wherein the molar ratio of base to 1-naphthyl-2-aminoethylketone acid salt is at least 0.7, b) addition of hydrazine to obtain a 3-(1-naphthyl)-1H-pyrazoline, c) optionally adding a second solvent and/or at least partially removing the first solvent, and d) heating the reaction mixture to a temperature above 190° C. to obtain the compound of Formula (1). 3. Process according to claim 1 , wherein compound of Formula (2) is prepared from 1-acetylnaphthalene.4. Process according to claim 1 , wherein the molar ratio is from 0.95-1.1.5. Process according to claim 1 , wherein water is removed from the resulting solution of step a.6. Process according to claim 1 , wherein R-Rare hydrogen.7. Process according to claim 1 , wherein Rand Rare methyl.8. Process according to claim 1 , wherein the molar ratio of hydrazine to compound of Formula (2) is between 0.90-1.05.9. Process according to claim 1 , wherein the first solvent is selected from the group consisting of triethylene glycol claim 1 , sulfolan claim 1 , propylene carbonate claim 1 , ethylene glycol claim 1 , diethylene glycol claim 1 , methyl tert.-butyl ether claim 1 , dimethylformamide claim 1 , dimethylacetamide and chinolin.10. Process according to claim 1 , wherein the first solvent is capable of forming an azeotrope with compound of Formula (1).11. An azeotrope comprising a solvent and a compound of Formula (1).12. The azeotrope according to claim 11 , wherein the solvent is triethylene glycol.14. A process according to for synthesizing a pharmaceutically active compound by further converting the compound of Formula (1) to obtain the pharmaceutically active compound. The present invention relates to a process for the production ...

BLUE LIGHT BLOCKING SYSTEM CONTAINING PYRAZOLINE OR/AND PHENYLACRYLIC COMPOUNDS

A blue light blocking system including a pyrazoline compound of formula (I) or/and a phenylacrylic compound of formula (II) is provided. The compound of formula (I) or formula (II) can absorb most blue light of shorter wavelength that hurt eyes, but let that of the longer wavelength pass through, so that the transmitted light makes an excellent visual effect for human. The system can be applied to products such as optical films, optical lenses, goggles, skin care, lighting, coatings, adhesives, or panels. These products have a light-colored appearance and their transmitted light makes for an excellent visual effect. 2. (canceled)4. The blue light blocking system according to claim 1 , whereinthe compound of the formula (I) or formula (II) is used separately.5. The blue light blocking system according to claim 1 , wherein claim 1 ,the compound of formula (I) and the compound of formula (II) are used in combination, and a mass ratio of the compounds ranges from 1:5 to 5:1.6. A blue light blocking composition for preparing the blue light blocking layer of claim 1 , comprisingat least a compound selected from formula (I) and/or formula (II), and polymerizable monomers or polymers.7. The blue light blocking composition according to claim 6 , comprisingat least a compound selected from formula (I) and/or formula (II), an initiator or initiators, and polymerizable monomers and/or prepolymers.8. The blue light blocking composition according to claim 6 , wherein claim 6 ,the monomer includes one or more acrylic, acrylic ester, methacrylic, methacrylic ester, hydroxyacrylic, methacrylic, vinyl, styrene, diene, vinyl fluoride, chlorine ethylene, acrylonitrile, vinyl acetate, silicone acrylate, epoxy acrylate, polyurethane acrylate, ethylene oxide, isocyanate, polyol, polythiol, polyamine amine, alcohol amine, and thiol amine.9. The blue light blocking composition according to claim 6 , further comprisingone or more auxiliaries selected from stabilizer, UV absorber, leveling ...

Targeting GLI Proteins in Human Cancer by Small Molecules

The present disclosure provides compositions, pharmaceutical preparations and methods for the diagnosis and treatment of cancers expressing a GLI polypeptide. The disclosed compositions and pharmaceutical preparations may comprise one or more pyrazolyl-containing compounds, or an analog or derivative thereof. 2. The compound of claim 1 , wherein Xis N and Xis C.3. The compound of claim 1 , wherein Xis C and Xis N.4. The compound of claim 1 , wherein Ris aryl.5. The compound of claim 1 , wherein Ris selected from aryl claim 1 , substituted aryl claim 1 , heteroaryl claim 1 , and alkyl.6. The compound of claim 1 , wherein Ris selected from heteroaryl and alkyl.7. The compound of claim 1 , wherein Ris aryl.8. The compound of claim 1 , wherein Ris substituted aryl.9. The compound of claim 1 , wherein Ris hydrogen.10. The compound of claim 1 , wherein Y is C-Calkyl and Z is C-Calkyl.11. The compound of claim 10 , wherein Y is C-Calkyl and Z is C-Calkyl claim 10 , such that Y and Z form —(CH)—C(CH)—CH—.12. The compound of claim 1 , wherein Y is C-Calkyl and Z is aryl.14. The compound of claim 1 , wherein Ris aryl claim 1 , Ris heteroaryl claim 1 , and Ris aryl.15. The compound of claim 1 , wherein Ris aryl claim 1 , Ris alkyl claim 1 , and Ris substituted aryl.16. The compound of claim 1 , wherein Ris aryl claim 1 , Ris aryl claim 1 , and Ris aryl.17. The compound of claim 1 , wherein Ris aryl claim 1 , Ris substituted aryl claim 1 , and Ris substituted aryl.23. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) the compound of ; and'}(ii) a pharmaceutically acceptable carrier.24. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) the compound of ; and'}(ii) a chemotherapeutic agent.25. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) the compound of ; and'}(ii) a therapeutic agent selected from erlotinib, pemetrexed, LY294002, SB431542, ...

CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING DISEASE CONDITIONS, INCLUDING METABOLIC DISORDERS AND CANCERS

The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers. 2. A compound of claim 1 , wherein the compound is Example 1 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.3. A compound of claim 2 , wherein the stereomeric purity is at least 95%.4. A compound of claim 1 , wherein the compound is Example 2 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.5. A compound of claim 4 , wherein the stereomeric purity is at least 95%.6. A compound of claim 1 , wherein the compound is Example 3 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.7. A compound of claim 6 , wherein the stereomeric purity is at least 95%.8. A compound of claim 1 , wherein the compound is Example 4 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.9. A compound of claim 7 , wherein the stereomeric purity is at least 95%.10. A pharmaceutical composition claim 1 , comprising: a therapeutically effective amount of a compound of and a pharmaceutically acceptable carrier.11. A method of treating a disease claim 1 , comprising: administering to a mammal in need thereof a therapeutically effective amount of a compound of claim 1 , wherein the disease is selected from obesity claim 1 , diabetes claim 1 , dyslipidemias claim 1 , cardiovascular disorders claim 1 , inflammatory disorders claim 1 , hepatic disorders claim 1 , cancers claim 1 , and a combination thereof.12. The method of claim 11 , wherein the diabetes disorder is selected from Type 1 diabetes claim 11 , Type 2 diabetes claim 11 , inadequate glucose tolerance claim 11 , and insulin resistance.13. ...

CANNABINOID RECEPTOR MEDIATING COMPOUNDS

A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CBreceptor mediating scaffold conjugated to (ii) a second therapeutic scaffold. 2. The compound of claim 1 , wherein Rand Rare each independently selected from H claim 1 , hydroxy claim 1 , C-Calkyl claim 1 , or acyl.3. The compound of claim 1 , wherein Ris C-Calkyl claim 1 , C-Ccycloalkyl claim 1 , amino claim 1 , phenyl claim 1 , heteroaryl claim 1 , acyl or heterocycloalkyl.4. The compound of claim 1 , wherein Rand Rare each H.5. The compound of claim 1 , wherein a and c are each one claim 1 , Ris halogen claim 1 , and Ris halogen.6. The compound of claim 1 , wherein b is zero.7. The compound of claim 1 , wherein X is SO.10. The compound of claim 9 , wherein Ris methyl or —NH(acetamido) and Ris CFor Cl.12. The compound of claim 11 , wherein Ris H claim 11 , acyl claim 11 , or C-Calkyl.14. The compound of claim 1 , wherein the compound has a plasma half-life of 4 to 8 hours.15. The compound of claim 1 , wherein the compound preferentially targets CBreceptors in peripheral tissue claim 1 , while not interacting with CBreceptors in brain tissue.16. A pharmaceutical composition comprising a compound of claim 1 , and at least one pharmaceutically acceptable additive.17. A method for treating obesity claim 1 , diabetes claim 1 , non-alcoholic and alcoholic fatty liver disease claim 1 , a co-morbidity of obesity claim 1 , dyslipidemias that predispose to arteriosclerotic heart disease claim 1 , diabetic nephropathy claim 1 , gout claim 1 , fibrosis claim 1 , or liver cancer in a subject claim 1 , or reversing insulin resistance in a subject claim 1 , comprising administering to the subject in need thereof a therapeutically effective amount of a compound of .18. The method of claim 17 , comprising treating obesity in the subject.19. The method of claim 17 , comprising treating diabetes in the subject.20. A method of preventing or reversing the deposition of adipose tissue in a subject ...

4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVE OR SALTS THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

The present invention provides a 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt effectively increases the LXR transcriptional activity, and therefore can be usefully applied for preventing or treating a dysfunction in cholesterol metabolism, such as cholesterol gallstone, hyperlipidemia, or coronary atherosclerosis. 2. The compound or its pharmaceutically acceptable salt of claim 1 , wherein Ring Y is benzene.3. The compound or its pharmaceutically acceptable salt of claim 1 , wherein Ring Y is pyridine.4. The compound or its pharmaceutically acceptable salt of claim 1 , wherein Ring Y is thiophene.5. The compound or its pharmaceutically acceptable salt of claim 1 , wherein Ris CFCF.7. The compound or its pharmaceutically acceptable salt of claim 5 , wherein Ris hydrogen.8. The compound or its pharmaceutically acceptable salt of claim 5 , wherein Ris halogen; and Ring X and Ring Y are benzene.10. The compound or its pharmaceutically acceptable salt of claim 1 , wherein Ris C(CF)OH.12. The compound or its pharmaceutically acceptable salt of claim 10 , wherein Ris hydrogen.13. The compound or its pharmaceutically acceptable salt of claim 10 , wherein Ris halogen; and Ring X and Ring Y are benzene.14. The compound or its pharmaceutically acceptable salt of claim 10 , wherein Ris hydrogen; Ris halogen; Ring X and Ring Y are benzene; Ris a phenyl group claim 10 , a pyridinyl group claim 10 , a 1 claim 10 ,2 claim 10 ,3 claim 10 ,6-tetrahydropyridinyl group claim 10 , or a piperazinyl group (where the phenyl group claim 10 , the pyridinyl group claim 10 , the 1 claim 10 ,2 claim 10 ,3 claim 10 ,6-tetrahydropyridinyl claim 10 , or the piperazinyl group is optionally substituted with one or more substituents selected from the group consisting of C˜Calkylthio; C˜Calkylsulfonyl; ...

PYRAZOLINE DERIVATIVES AS INSECTICIDAL COMPOUNDS

The present invention relates to compounds of formula I This application is a divisional application of U.S. patent application Ser. No. 14/762,319, filed Jul. 21, 2014 which is a 371 filing of International Application No. PCT/CN2014/071207, filed Jan. 23, 2014, which claims priority benefit to International Application No. PCT/CN2013/070902 filed Jan. 23, 2013, the contents of all of which are incorporated herein by reference.The present invention relates to certain pyrazoline derivatives, to processes and intermediates for preparing these derivatives, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these derivatives and to methods of using these derivatives to control insect, acarine, nematode and mollusc pests.Certain isoxazoline derivatives with insecticidal properties are disclosed, for example, in EP 1,731,512. However there is a continuing need to find new biologically active compounds as well as new biologically active compounds displaying superior properties for use as agrochemical active ingredients, for example greater biological activity, different spectrum of activity, increased safety profile, or increased biodegradability.It has now surprisingly been found that certain pyrazoline derivatives have highly potent insecticidal properties.The present invention provides compounds of formula (I)whereinP is selected from P1 and P2, or P and Rtogether are P3or P is a heterocycle H, selected from H1 to H9Y, Y, and Yare independently of each other C—H, C—R, or nitrogen;Gis oxygen or sulfur;Gis oxygen or sulfur;Gis oxygen or sulfur;Ris hydrogen, C-Calkyl, C-Calkoxy, C-Calkylcarbonyl, or C-Calkoxycarbonyl;Ris C-Calkyl or C-Calkyl substituted by one to five R, C-Ccycloalkyl or C-Ccycloalkyl substituted by one to five R, C-Ccycloalkyl-C-Calkylene or C-Ccycloalkyl-C-Calkylene substituted by one to five R, aryl-C-Calkylene- or aryl-C-Calkylene- substituted by one to five R, heterocyclyl-C-Calkylene- or heterocyclyl-C-Calkylene- ...

Organic Scintillators Derived from Pyrazoline

Pyrazoline-based fluorophores and plastic scintillators incorporating the fluorophores are described. The fluorophores include 1,3,5-triaryl substituted pyrazolines. A fluorophore of a plastic scintillator can be a 1-phenyl-4,5-1H-dihydroyrazole having the structure: 1. A plastic scintillator comprising a polymeric matrix and a 1 ,3 ,5-triaryl substituted pyrazoline incorporated in the polymeric matrix.4. The plastic scintillator of claim 3 , wherein Ris sulfur and Ris oxygen.6. The plastic scintillator of claim 5 , wherein Ris an aryl bromide or an aryl fluoride.8. The plastic scintillator of claim 1 , wherein the 1 claim 1 ,3 claim 1 ,5-triaryl substituted pyrazoline is bonded to a polymer of the polymeric matrix.9. The plastic scintillator of claim 8 , wherein the 1 claim 8 ,3 claim 8 ,5-triaryl substituted pyrazoline is bonded to a chain of the polymer via reaction of reactive functional group of the pyrazoline with a reactive group of the polymer.10. The plastic scintillator of claim 8 , wherein the 1 claim 8 ,3 claim 8 ,5-triaryl substituted pyrazoline is bonded to the polymer via reaction of a bifunctional crosslinking agent with a reactive functional group of the pyrazoline and with a reactive group of the polymer.11. The plastic scintillator of claim 10 , wherein the 1 claim 10 ,3 claim 10 ,4-triaryl substituted pyrazoline has been copolymerized with the bifunctional crosslinking agent via chain polymerization or step polymerization.12. The plastic scintillator of claim 1 , wherein the polymeric matrix comprises a polystyrene.13. The plastic scintillator of claim 1 , wherein the polymeric matrix comprises a polyvinyltoluene or a polyvinylcarbazole14. The plastic scintillator of claim 1 , further comprising a second fluorophore.15. The plastic scintillator of claim 1 , wherein the plastic scintillator is free of any secondary fluorophores.17. The fluorophore of claim 16 , wherein Ris an aryl halide.19. The fluorophore of claim 16 , wherein Ris a phenyl ...

PYRAZOLINE DERIVATIVES AS INSECTICIDAL COMPOUNDS

The present invention relates to compounds of formula (I) wherein P is selected from P1 and P2, or P and Rtogether are P3 or P is a heterocycle H, selected from H1 to H9 wherein Y, Yand Yare independently of each other C—H, C—R, or nitrogen; and G, G, G, Z, R, R, R, R, R, R, R, R, R, R, R, R, p, n and k are as defined in the claims. The invention also relates to methods of controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I). 2. A compound according to claim 1 , wherein P is P1.3. A compound according to claim 1 , wherein P is P2.4. A compound according to claim 1 , wherein P and Rtogether are P3.5. A compound according to claim 1 , wherein P is a heterocycle H claim 1 , selected from H1 to H9.6. A compound according to claim 1 , wherein Yis C—H or nitrogen claim 1 , Yand Yare independently C—H or nitrogen; wherein no more than two of Y claim 1 , Yand Yare nitrogen and wherein Yand Yare not both nitrogen.7. A compound according to claim 1 , wherein G claim 1 , Gand Gare oxygen;8. A compound according to claim 1 , wherein Ris chlorodifluoromethyl or trifluoromethyl.10. A compound according to claim 1 , wherein Ris hydrogen claim 1 , chloro claim 1 , bromo claim 1 , fluoro claim 1 , methyl or trifluoromethyl.12. A method of controlling insects claim 1 , acarines claim 1 , nematodes or molluscs which comprises applying to a pest claim 1 , to a locus of a pest claim 1 , or to a plant susceptible to attack by a pest an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in .13. An insecticidal claim 1 , acaricidal claim 1 , nematicidal or molluscicidal composition comprising an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount ...

CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING METABOLIC DISORDERS, INCLUDING OBESITY AND DIABETES

The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers. 2. The method of claim 1 , wherein the compound is Example 1 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.3. The method of claim 2 , wherein the stereomeric purity is at least 95%.4. The method of claim 1 , wherein the compound is Example 2 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.5. The method of claim 4 , wherein the stereomeric purity is at least 95%.6. The method of claim 1 , wherein the compound is Example 3 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.7. The method of claim 6 , wherein the stereomeric purity is at least 95%.8. The method of claim 1 , wherein the compound is Example 4 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 60%.987. The method of claim claim 1 , wherein the stereomeric purity is at least 95%.10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. (canceled)20. The method of claim 1 , wherein the compound is Example 1 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 90%.21. The method of claim 20 , wherein the stereomeric purity is at least 99%.22. The method of claim 1 , wherein the compound is Example 2 or a pharmaceutically acceptable salt thereof claim 1 , wherein the stereomeric purity is at least 90%.23. The method of claim 22 , wherein the stereomeric purity is at least 99%.24. The method of claim 1 , wherein the compound is Example 3 or a pharmaceutically acceptable salt thereof claim 1 , wherein the ...

ORGANIC COMPOUNDS

The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders. 2. The compound according to claim 1 , wherein Ris aryl optionally substituted with one or more groups selected from Calkyl claim 1 , Ccycloalkyl claim 1 , Calkoxy and haloCalkyl claim 1 , in free or salt form.3. The compound according to claim 1 , wherein Ris Calkyl claim 1 , in free or salt form.5. A pharmaceutical composition comprising a compound according to claim 1 , in combination or association with a pharmaceutically acceptable diluents or carrier.6. A method for the treatment of a PDE2 mediated disorder comprising administering to a subject in need thereof an effective amount of a compound according to .7. The method of claim 6 , wherein the disorder is selected from the group consisting of neurological disorders; cerebrovascular diseases; spinal muscular atrophy; lateral sclerosis; multiple sclerosis; cognitive disorders; cognitive dysfunction associated with Parkinson's disease and depression; mental deficiency; sleep disorders; psychiatric disorders factitious disorder; impulse control disorders; mood disorders; psychomotor disorders; psychotic disorders; drug dependence; eating disorders; pediatric psychiatric disorders; mental and behavioral disorders due to psychoactive substance use; cardiovascular disorder; and pain.8. The method of wherein the disorder is selected from the group consisting-of: anxiety claim 6 , depression claim 6 , autism spectrum disorder claim 6 , schizophrenia claim 6 , anxiety and/or depression in autistic and/or schizophrenic patients claim 6 , and cognitive impairment associated with schizophrenia or dementia.9. (canceled)10. A pharmaceutical composition comprising the compound according to claim 1 , in pharmaceutically acceptable salt form.11. A pharmaceutical composition comprising the compound according to claim 4 , in ...

CANNABINOID RECEPTOR MEDIATING COMPOUNDS

A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CBreceptor mediating scaffold conjugated to (ii) a second therapeutic scaffold. 2. The compound of claim 1 , wherein Rand Rare each independently selected from H claim 1 , hydroxy claim 1 , C-Calkyl claim 1 , or acyl.3. The compound of claim 1 , wherein Ris C-Calkyl claim 1 , C-Ccycloalkyl claim 1 , amino claim 1 , phenyl claim 1 , heteroaryl claim 1 , acyl or heterocycloalkyl.4. The compound of claim 1 , wherein Rand Rare each H.5. The compound of claim 1 , wherein a and c are each one claim 1 , Ris halogen claim 1 , and Ris halogen.6. The compound of claim 1 , wherein b is zero.7. The compound of claim 1 , wherein X is SO.10. The compound of claim 9 , wherein Ris methyl or —NH(acetamido) and Ris CFor Cl.12. The compound of claim 11 , wherein Ris H claim 11 , acyl claim 11 , or C-Calkyl.14. A pharmaceutical composition comprising a compound of claim 1 , and at least one pharmaceutically acceptable additive.15. A method for treating obesity claim 1 , diabetes claim 1 , non-alcoholic and alcoholic fatty liver disease claim 1 , a co-morbidity of obesity claim 1 , dyslipidemias that predispose to arteriosclerotic heart disease claim 1 , diabetic nephropathy claim 1 , gout claim 1 , fibrosis claim 1 , or liver cancer in a subject claim 1 , or reversing insulin resistance in a subject claim 1 , comprising administering to the subject in need thereof a therapeutically effective amount of a compound of .16. The method of claim 15 , comprising treating obesity in the subject.17. The method of claim 15 , comprising treating diabetes in the subject.18. A method of preventing or reversing the deposition of adipose tissue in a subject claim 1 , comprising administering to the subject in need thereof an effective amount of a compound of .19. The method of claim 15 , wherein administering of the compound causes substantially no adverse neuropsychiatric effects.20. The method of claim 15 , wherein ...

Electrophotographic receptor

USE OF BROMOPHENOL-PYRAZOLINE COMPOUNDS FOR THE TREATMENT OF FELINE CORONAVIRUS DISEASES

The present invention belongs to the field of medical technology, and specifically relates to use of bromophenol-pyrazoline compounds for the treatment of feline coronavirus diseases. Studies carried out for the present invention revealed that bromophenol-pyrazoline compounds could inhibit activity of feline infectious peritonitis virus main protease (FIPV M) and interfere with replication of feline infectious peritonitis virus (FIPV) in cells. In a clinical trial, the bromophenol-pyrazoline compounds can treat infectious peritonitis in cats naturally infected with the FIPV, greatly improve survival rate of cats, and can be used to prepare drugs for treating feline infectious peritonitis. 2. The use according to claim 1 , wherein the feline coronavirus diseases are feline infectious peritonitis caused by feline infectious peritonitis virus (FIPV). The present invention belongs to the field of medical technology, and relates to a new use of bromophenol-pyrazoline compounds, in particular use of bromophenol-pyrazoline compounds for the prevention/treatment of feline coronavirus diseases.Feline coronavirus (FCV), belonging to nido-viridae of coronaviridae, is an enveloped, non-segmented, single-stranded positive-strand RNA virus. Feline enteric coronavirus (FECV) is the most common FCV, is ubiquitous in cats worldwide, can be transmitted through fecal-oral route, but is not a serious pathogen itself. Approximately 5% of cats persistently infected with the FECV develop a highly lethal mutant feline infectious peritonitis virus (FIPV). The FIPV resulting from mutation of the FECV lose the ability to infect healthy cats, but has greatly increased pathogenicity and lethality.The FIPV can replicate efficiently and sustainably in mononuclear phagocytes, and expand throughout the body as the mononuclear phagocytes circulate in the body, causing the host cat's immune system hyperreponsiveness, thus resulting in attack of diseases and death. Common sites of lesions of feline ...

一类含萘环和吡唑啉结构的硫脲类衍生物及其制法

一类含萘环和吡唑啉结构的硫脲类衍生物，其特征是它有如下通式： 结构式中R 1 为如下基团之一： R 2 为如下基团之一：

Pyrazoline-based sensitizers and manufacturing method and application thereof

피라졸린계 증감제 및 이의 제조방법과 응용이 개시된다. 상기 피라졸린계 증감제는 화학식 (I) 또는 화학식 (Ⅱ)에 도시된 구조를 가지며, 흡수 밴드는 350-440nm 사이에 존재하며, 광경화 시스템, 특히 디이미다졸 광개시제를 함유한 시스템중에 사용되기에 적합하며, 화학식 (I), 화학식 (Ⅱ)는 순차적으로 아래와 같다. Pyrazoline sensitizers and methods for their preparation and applications are disclosed. The pyrazoline-based sensitizers have the structure shown in formula (I) or formula (II) and the absorption bands are between 350-440 nm and are used in photocuring systems, especially those containing diimidazole photoinitiators. Formula (I) and Formula (II) are sequentially as follows.

Process for preparing 1-acyl-2-pyrazoline derivatives

1-Acyl-2-pyrazoline derivs. (II) are produced by cyclising by heating acylhydrazone derivs. (I) where R1= H, pyridyl, pyrazinyl, alkyl acyl (phenyl or phenyl substd. by lower alkyl) a halogen atom(s) or alkoxy; R2, R3 and R4= (independently) H, furyl, pyridyl, alkyl or acyl. Acylhydrazones (I) are easier to synthesise and more stable than an alternative starting material, 2-pyrazoline derivs., which are reacted with an acid chloride or anhydride to produce cpds. (II). Cpds. (II) are drugs for the treatment of cerebral edema.

Method of producing derivatives of 1-carbomoyl-2-pyrazoline

The invention relates to a herbicidally active compound of the general wherein R₁, R₂, R₃ and R₄ are equal or different and repre;sent hydrogen atoms, alkyl groups having 1-6 carbon atoms, cycloalkyl groups having 3-6 carbon atoms or alkoxycar­bonyl groups having 2-5 carbon atoms; R₅ is a hydrogen atom, an alkyl group or haloalkyl group having 1-8 carbon atoms, a substituted or non-substitu­ted phenyl group, a substituted or non-substituted heterocyclic group, or an alkenyl, alkynyl or alkoxy­carbonyl group having 2-5 carbon atoms; and wherein two of the groups R₁, R₂, R₃, R₄ and R₅ together may form a straight or branched alkylene group having 3-5 carbon atoms; Ar is a phenyl group, a phenyl(C₁-C₄)alkyl group or a heteroaryl group; R₆ is a hydrogen atom or substituent to Ar, which substituent, in case Ar is a phenyl or phenylalkyl group, is attached to the phenyl group in the ortho position with respect to the sulphonyl or sulphonylal­kyl group, and which substituent is selected from the following atoms and groups: a halogen atom; a nitro group; an alkoxycarbonyl group that has 2-8 carbon atoms and is unsubstituted or substituted with one or more hydroxy or C₁-C₄ alkoxy groups; and an alkyl, hydroxyalkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulphonyl and haloalkylsulphonyl group having 1-6 carbon atoms; and R₇ represent a hydrogen atom or one or two halogen atoms or C₁-C₄ alkyl groups.

The method of obtaining derivatives of 3-amino-2-pyrazoline

Cycloalkane-substituted pyrazoline compounds, their preparation and use as medicaments

The present invention relates to Cycloalkane-substituted substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.

Pyrazoline-based sensitizer, its preparation method and its application

피라졸린계 증감제 및 이의 제조방법과 응용이 개시된다. 상기 피라졸린계 증감제는 화학식 (I) 또는 화학식 (Ⅱ)에 도시된 구조를 가지며, 흡수 밴드는 350-440nm 사이에 존재하며, 광경화 시스템, 특히 디이미다졸 광개시제를 함유한 시스템중에 사용되기에 적합하며, 화학식 (I), 화학식 (Ⅱ)는 순차적으로 아래와 같다.

Patent FR2377386B1

1- (4-cyanophenylcarbamoyl) pyrazoline

본 발명은 살충 및 살비 활성을 지닌 하기 식의 피라졸린 유도체에 관한 것이다. 상기식에서, X 및 Y는 같거나 다르며, 불소 원자, 또는 할로겐으로 치환될 수 있는 C 1-4 -알킬기이고, R은 수소 원자, 또는 불소로 치환될 수 있는 C 1-4 -알킬기이다.

Use of phenylpyrazolin-3-carboxylates for improving plant yield

Compounds (A) can be used for increasing the yield of useful plants or crop plants with respect to their harvested plant organs, wherein the Compound (A) is selected from compounds of the formula (I) or salts thereof, in which (R 1 )n is n radicals R 1 where the R 1 are identical or different and are each halogen or (C 1 -C 4 )-haloalkyl, n is an integer from 1 to 3, R 2 is hydrogen, (C 1 -C 6 )-alkyl, (C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, (C 3 -C 6 )-cycloalkyl, tri-(C 1 - C 4 )-alkyl-silyl or tri-(C 1 -C 4 )-alkyl-silylmethyl, R 3 is hydrogen, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 2 -C 6 )-alkynyl or (C 3 -C 6 )-cycloalkyl, and R 4 is hydrogen or (C 1 -C 12 )-alkyl, preferably mefepyr-diethyl (Compound (A1 )].

Azoline compounds for combating invertebrate pests

The present invention relates to azoline compounds of formula (I) which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.

PEST CONTROL METHODS IN SOYA

La invención proporciona un método que comprende aplicar a un cultivo de plantas de soja, al locus de dichas plantas o su material de propagación un compuesto de la fórmula I donde X es P1 o P2 R5 es cloro, bromo, CF3 o metilo, p es 1, 2 o 3 y donde el método es para controlar y/o prevenir la infestación del cultivo de soja por parte de Euschistus , preferentemente Euschistus heros.

Use of mefenpyr-diethyl for controlling phytopathogenic fungi

The present invention relates to the use of mefenpyr-diethyl for controlling phytopathogenic fungi. Further the invention relates to methods for controlling phytopathogenic fungi, wherein the fungi, their habitat, their locus, or the plants, the soil or plant propagation material are treated with an effective amount of a composition comprising mefenpyr-diethyl.

Pyrazole-4- carboxamide derivatives as microbiocides

Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.

Pyrazole-4-carboxamide derivatives as microbiocides

Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.

ANTRANILAMIDE COMPOSITE, COMPOSITION THAT INCLUDES IT AND METHOD FOR CONTROLLING AN INVERTEBRATE PEST

Un compuesto de antranilamida seleccionado entre un compuesto de la Fórmula (1) o un N-óxido del mismo donde R1 es CH3, F, Cl o Br; R2 es F, Cl, Br, I o CF3; R3 es CF3, Cl, Br o OCH2CF3; R4a es alquilo C1-4; R4b es H o CH3; y R5 es Cl o Br; o una sal aceptable para uso en la agricultura del mismo. También se describen las composiciones que comprenden a estos compuestos y el método para controlar plagas de invertebrados tales como artrópodos en entornos agronómicos, tales como cultivos almacenados y en crecimiento y en entornos no agronómicos tales como forestación, cultivos de invernadero, plantas ornamentales, cultivos de vivero, alimentos almacenados y productos de fibra, en el ganado, en el hogar, en la salud pública y en animales. An anthranilamide compound selected from a compound of Formula (1) or an N-oxide thereof where R1 is CH3, F, Cl or Br; R2 is F, Cl, Br, I or CF3; R3 is CF3, Cl, Br or OCH2CF3; R4a is C1-4 alkyl; R4b is H or CH3; and R5 is Cl or Br; or an acceptable salt for use in agriculture thereof. Compositions comprising these compounds and the method for controlling invertebrate pests such as arthropods in agronomic environments, such as stored and growing crops and in non-agronomic environments such as afforestation, greenhouse crops, ornamental plants, crops of crops are also described. nursery, stored food and fiber products, in livestock, at home, in public health and in animals.

3--45--1- method for preparing 3-halo-45-dihydro-1h-pyrazoles

본 발명은 하기 화학식 (II)의 4,5-디히드로-1H-피라졸 화합물을 화학식 HX 1 의 화합물과 접촉시키는 것을 포함하는, 하기 화학식 (I)의 3-할로-4,5-디히드로-1H-피라졸 화합물의 제조 방법에 관한 것이다. 하기 식에서 X 1 은 할로겐이고, L, R, k 및 X 2 는 본원에서 정의된 바와 같다. 본 발명은 또한 X 1 , R 3 , R 6 , R 7 , R 8a , R 8b 및 n이 본원에 정의된 바와 같은 하기 화학식 (III)의 화합물의 제조를 개시한다. The present invention comprises contacting a 4,5-dihydro-1H-pyrazole compound of formula (II) with a compound of formula HX 1 , wherein 3-halo-4,5-dihydro of formula (I) A method for producing a -1H-pyrazole compound. Wherein X 1 is halogen and L, R, k and X 2 are as defined herein. The invention also discloses the preparation of compounds of formula (III), wherein X 1 , R 3 , R 6 , R 7 , R 8a , R 8b and n are as defined herein. <화학식 I> <Formula I> <화학식 II> <Formula II> <화학식 III> <Formula III> 3-할로-4,5-디히드로-1H-피라졸, 4,5-디히드로-1H-피라졸, 할로겐 3-halo-4,5-dihydro-1H-pyrazole, 4,5-dihydro-1H-pyrazole, halogen

Charge transport cpd. for electrostatographic recording material - is di:aryl styryl pyrazoline cpd., to give high speed and low residual potential without fatigue

Charge transporting substance (I) used in an electrostatographic recording material, having a conductive substrate with a coating based on (I) and a high mol. binder (II), is a 2,5-diaryl-2-styryl-pyrazoline cpd. of formula: (in which R1-3 are opt. substd. aryl gps.). Pref. R1-3 are phenyl, opt. with an amino, di(ar)alkylamino, diarylamino, alkylarylamino, morpholino, piperazino, piperidino or alkoxy gp. in the 4-posn. The material also contains a charge-producing substance (III) in the same or an adjacent layer, (III) pref. being an inorganic photoconductor or an organic dyestuff or pigment. (II) is a (meth)acrylic, polycarbonate, polyester, PVC, vinylidiene chloride-acrylonitrile copolymer, PVDC and/or phenol-HCHO resin. (II) is used in an amt. of 0.8-4 (wt.) pts./pt. (I). The (I) layer is 5-30 mu m thick and the (III) layer 0.05-5 (0.1-3) mu m thick. The material does not suffer fatigue and has high speed and low residual potential when used repeatedly. The (I) layer has high homogeneity and film strength and excellent stability.

Electrophotographic recording material

Es wird ein elektrophotographisches Aufzeichnungsmaterial beschrieben aus einem elektrisch leitenden Schichtträger und mindestens einer bindemittelhaltigen photoleitfähigen Schicht, die ein Perylentetracarbonsäurederivat als Ladungsträger erzeugende Verbindung und ein Hydrazon- bzw. Pyrazolinderivat als Ladungen transportierende Verbindung enthält, bei dem die Ladungsträger erzeugende Verbindung ein Perylentetracarbonsäurediimid ist und die Ladungen transportierende Verbindung der allgemeinen Formel $F1 entspricht, in der X - Methyl oder Methoxyl n - Null oder 1 Y - Phenyl und Z - Wasserstoff oder Y und Z - die Gruppierung $F2 mit A-Phenyl oder p-Tolyl bedeuten.

Material for electrophotographic reproduction

Synthetic method of mefenpyr-diethyl

本发明涉及一种吡唑解草酯的合成方法。该方法包括：将2,4‑二氯苯肼盐酸盐、乙醛酸乙酯和碱在溶剂中反应，将得到的2,4‑二氯苯肼乙醛酸乙酯腙与甲基丙烯酸乙酯在催化剂和氧化剂作用下，在溶剂中发生[3+2]环加成反应。该方法起始原料易得，缩短了反应时间，反应路线短，成本低，操作简单，降低了三废处理，且同样收率较高，易于工业化生产。

Phosphorus compound

Electrophotographic recording material

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

HYDRAZIDE COMPOUND AND ITS APPLICATION FOR PEST CONTROL

1. Соединение гидразида, представленное формулой (1):где G представляет 5-членную гетероциклическую группу, представленную следующей формулой G-1, G-2 или G-3:гдеикаждая представляет связь, исвязана с фрагментомв формуле (1),Rпредставляет C1-C4 галогеналкильную группу,Yпредставляет атом кислорода, атом серы или группу NR,Yпредставляет атом кислорода, атом серы, группу NRили метиленовую группу,Yпредставляет атом кислорода, атом серы, группу NRили метиленовую группу,Rпредставляет C1-C6 алкильную группу, C2-C6 алкенильную группу, C2-C6 алкинильную группу, C3-C6 циклоалкильную группу, C4-C7 циклоалкилалкильную группу, C2-C6 алкилкарбонильную группу, C2-C6 алкоксикарбонильную группу, C2-C6 алкиламинокарбонильную группу, C3-C9 диалкиламинокарбонильную группу, фенильную группу, цианогруппу, формильную группу или атом водорода,M представляет атом кислорода или атом серы,Q, Q, Qи Qнезависимо представляют атом азота или группу CR,Rпредставляет необязательно галогенированную C1-C6 алкильную группу, необязательно галогенированную C1-C6 алкоксильную группу, нитрогруппу, цианогруппу, атом галогена или атом водорода,m представляет целое число от 0 до 5,Rпредставляет необязательно галогенированную C1-C6 алкильную группу, необязательно галогенированную C1-C6 алкоксильную группу, C1-C6 алкилтиогруппу, C1-C6 алкилсульфинильную группу, C1-C6 алкилсульфонильную группу, нитрогруппу, цианогруппу или атом галогена,при условии, что когда m является целым числом от 2 до 5, группы Rмогут быть одинаковыми или отличаться друг от друга,Rи Rнезависимо представляют углеводородную группу с цепью С1-С12, необязательно замещенную с помощью группы, выбранной из группы Е1, бензоильную группу, нео� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 207/18 (13) 2011 136 823 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2011136823/04, 05.02.2010 (71) Заявитель(и): СУМИТОМО КЕМИКАЛ КОМПАНИ, ЛИМИТЕД (JP) Приоритет(ы): (30) Конвенционный приоритет: ...

The method of obtaining 3-amino-2-pyrazoline derivatives or their salts

Method for producing 3-amino-pyrazoline derivatives

Medicinal uses of dihydropyrazoles

Compounds having a structure according to Formula (I): are effective in a method of increasing erythropoietin and vascularization of tissue in a subject in need thereof.

Method of optical bleaching of textile

TRANSFORMATION OF 2-PYRAZOLINES TO PYRAZOLES USING BROMINE

1. Способ получения соединения формулы 1 ! ! где Х представляет Н, галоген, OR3 или необязательно замещенную углеродную группу, ! L представляет необязательно замещенную углеродную группу, ! R1 представляет Н или необязательно замещенную углеродную группу, ! R2 представляет Н, необязательно замещенную углеродную группу, NO2 или SO2R4, ! R3 представляет Н или необязательно замещенную углеродную группу и ! R4 представляет необязательно замещенную углеродную группу, ! включающий: ! контактирование 2-пиразолина формулы 2 ! ! с бромом при температуре по меньшей мере приблизительно 80°С. ! 2. Способ по п.1, где ! Х представляет галоген, OR3 или С1-С4 галогеналкил, ! L представляет фенильное кольцо или 5- или 6-членное гетероароматическое кольцо, необязательно замещенное 1-3 R5, ! R1 представляет Н, ! R2 представляет Н, CN, С1-С4 алкил, СО2R10, NO2 или SO2R4, ! R3 представляет Н или С1-С4 галогеналкил, ! R4 представляет С1-С4 алкил или необязательно замещенный фенил, ! каждый R5 независимо представляет галоген или С1-С4 галогеналкил и ! R10 представляет Н или С1-С4 алкил. ! 3. Способ по п.2, где соединение формулы 1 представлено формулой 1а ! ! и соединение формулы 2 представлено формулой 2а ! ! где Z представляет N или CR9, ! R9 представляет Н, галоген или С1-С4 галогеналкил и ! n представляет целое число от 0 до 3. ! 4. Способ по п.3, где ! Х представляет Br или CF3 и ! Z представляет N, ! каждый R5 независимо представляет галоген или CF3 и ! R10 представляет метил или этил. ! 5. Способ по п.3, где ! Х представляет OR3, ! R3 представляет Н или С1-С4 галогеналкил и ! R10 представляет Н или С1-С4 алкил. ! 6. Способ по п.5, где ! Х представляет ОН, OCF2Н или OCH2CF3, ! Z представляет N, ! каждый R5 независимо представляет галоген или CF3 и ! R10 п� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2007 138 552 (13) A (51) МПК C07D 401/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2007138552/04, 14 ...

Insectocaricidal composition

Изобретение относитс  к химическому средству защиты растений от вредного воздействи  насекомых и клещей. Изобретение позвол ет повысить эффективность действи  предлагаемой композиции за счет того, что она содержит, мас.%: производные пиразолина формулы @ где X-OCH 2 CF 3 или OCH 2 @ , Y-CL или OCHF 2 20 This invention relates to a chemical plant protection agent against the harmful effects of insects and mites. The invention allows to increase the effectiveness of the proposed composition due to the fact that it contains, in wt%: pyrazoline derivatives of the formula @ where X-OCH 2 CF 3 or OCH 2 @, Y-CL or OCHF 2 20 изофорон 75 и смесь нонилфенилполиоксиэтилена с кальцийдодецилбензолсульфонатом 5. 7 табл. isophorone 75 and a mixture of nonylphenylpolyoxyethylene with calcium dodecylbenzenesulfonate 5. Table 7.

Process for preparing 4,5-dihydro-1H-pyrazole and intermediates

(S)-4,5-디하이드로-1H-피라졸 고리를 함유하는 화합물의 제조를 위한 확장 가능한 방법이 기재되어 있다. 이 방법은 선택한 키랄 분할제를 사용한 중간체의 키랄 분할 단계를 포함한다. 예를 들어, 키랄 분할제는 (-)-퀴닌, (R)-페네틸아민, (S)-페네틸아민, (S)-1-나프틸에틸아민, (R)-(-)-2-아미노-3-메틸-1-부탄올, (-)-신코니딘, (-)-스파르테인, (R)-1-나프틸에틸아민, D-아르기닌, L-리신, (S)-(+)-2-피롤리딘메탄올, 및 (1R,2S)-(+)-시스-1-아미노-2-인다놀로부터 선택될 수 있다.

Substituted carbamoylpyrazolines

본 발명은 일반식(I)의 신규한 치환된 카르바모일피라졸린, 그의 제조방법 및 농약으로서의 용도에 관한 것이다. 상기식에서, R 1 은 각각이 임의로 치환되고 질소를 통해 결합된 아졸리논, 아졸린티온 또는 아졸린이미노 래디칼을 나타내며, R 2 는 수소, 알킬, 임의로 치환된 시클로알킬, 할로게노아릴, 할로게노알킬티오 또는 알콕시카르보닐을 나타내고, R 3 은 수소, 알킬 또는 하기의 그룹을 나타내며, 여기에서, R 7 및 R 8 은 각 경우에 서로 독립적으로 수소, 알킬 또는 아릴을 나타내며, R 9 는 수소, 알킬 또는 아릴을 나타내고, n은 1 내지 6의 수를 나타내며, R 4 는 수소 또는 알킬을 나타내고, R 5 는 수소, 알킬, 페닐 또는 알킬티오를 나타내며, R 6 은 임의로 치환된 알킬, 임의로 치환된 시클로알킬 또는 하기의 래디칼을 나타내고, 여기에서, R 10 및 R 11 은 같거나 상이할 수 있으며, 수소, 할로겐, 알킬, 니트로, 시아노, 할로게노알킬, 알콕시, 할로게노알콕시, 알킬티오, 할로게노알킬티오, 임의로 치환된 페녹시, 임의로 치환된 모노-또는 디알킬아미노, 임의로 치환된 시클로알킬, 알콕시카르보닐, 임의로 치환된 아릴티오, 알케닐옥시, 알키닐, 알킬티오닐, 알킬설포닐, 할로게노알킬티오닐, 할로게노알킬설포닐 또는 할로게노알콕시카르보닐을 나타내거나, R 10 및 R 11 이 함께 임의로 하나 또는 두개의 산소 원자를 함유하며 임의로 치환된 2가 래디칼을 나타내고, X는 산소 또는 황을 나타내며, Y 및 Z는 같거나 상이할 수 있으며 수소, 알킬, 할로겐, 할로게노알킬, 알콕시, 알킬티오, 할로게노알콕시, 할로게노알킬티오, 알콕시카르보닐, 할로게노알콕시카르보닐, 임의로 치환된 아릴옥시, 임의로 치환된 아릴티오, 알케닐옥시, 알키닐, 알킬티오닐, 알킬설포닐, 할로게노알킬티오, 할로게노알킬설포닐, 니트로 또는 시아노를 나타내거나, Y 및 Z가 함께 각각이 임의로 할로겐으로 치환된 3,4-메틸렌디옥시 또는 3,4-에틸렌디옥시를 나타낸다.

The carbamoylpyrazolines that replaces

本发明涉及新的取代的氨基甲酰基吡唑啉、它们 的制备方法以及它们作为杀虫剂的应用。 其中R 1 、R 2 、R 3 、R 4 、R 5 、R 6 、X、Y和Z的定义同 说明书所述。

Fluorescent agent having ethynyl group

자외 ∼ 가시 단파장영역 (예를 들어, 350 ㎚ ∼ 420 ㎚) 에 높은 흡수성을 갖고, 분자 내에 에티닐기를 구비하는 일반식 (I) [화학식 1] (I) (식 중, R 1 , R 2 및 R 3 은 명세서에서 정의한 바와 같다) 로 나타내는 피라졸린 화합물로 대표되는 신규 형광제를 제공한다. (I) having high absorptivity in an ultraviolet to visible short wavelength region (for example, 350 nm to 420 nm) and having an ethynyl group in the molecule, [Chemical Formula 1] (I) (Wherein R 1 , R 2 and R 3 are as defined in the specification).

Preparation method of bromo-pyrazole carboxylic ester compound

本发明属于有机合成领域，具体地涉及一种溴代吡唑羧酸酯类化合物的制备方法。反应式如下，

The method of producing sulfamide derivatives-pyrazolin-1-carbonamide

Pyrazolic compound

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Substituted heterocyclic compounds and their use as fungicides

(57)【要約】 本発明は新規な置換された複素環式化合物、それらの複数の製造方法および殺菌・殺カビ剤としてのそれらの使用、並びに中間体、それらの複数の製造方法および殺菌・殺カビ剤としてのそれらの使用に関する。

Arthropodicidal anthranilamides

This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R 1 , R 2 , R 3 , R 4a , R 4b and R 5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.

Method for controlling particular insect pests by applying anthranilamide compounds

This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R 1 through R 8 are as defined in the disclosure. This invention further relates to a bezoxazinone compound of Formula 10 wherein R 4 through R 8 are as defined in the disclosure, useful for preparation of a compound of Formula I.

Arthropodicidal anthranilamides

This invention provides a composition comprising a biologically effective amount of a compound of Formula 1, an N-oxide or an agriculturally suitable salt thereof wherein R 1 , R 2 , R 3 , R 4a , R 4b and R 5 are as defined in the disclosure, and an effective amount of at least one fungicide.

Arthropodicidal anthranilamides

This invention provides a method for soil systemic control of an invertebrate pest by contacting the soil with a biologically effective amount of a compound of Formula 1, an N-oxide or an agriculturally suitable salt thereof wherein R 1 , R 2 , R 3 , R 4a , R 4b and R 5 are as defined in the disclosure.

Method of controlling particular insect pests by applying anthranilamide compounds

This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R 1 through R 8 are as defined in the disclosure. This invention further relates to a benzoxazinone compound of Formula 10 wherein R 4 through R 8 are as defined in the disclosure, useful for preparation of a compound of Formula I.

Anthranilamides compositions

This invention provides a compositions and methods of using biologically effective amount of a compound of Formula 1, an N-oxide or an agriculturally suitable salt thereof wherein R 1 , R 2 , R 3 , R 4a , R 4b and R 5 are as defined in the disclosure, to protect genetically modified plants and their environment. An effective amount of at least one additional biological agent can be combined with the compound of Formula 1.

Arthropodicidal anthranilamides

This invention provides a composition comprising a first compound selected from Formula 1, an N-oxide or an agriculturally suitable salt thereof; and a second compound selected from pyrethroids, wherein R 1 , R 2 , R 3 , R 4a , R 4b and R 5 are as defined in the disclosure.

Arthropodicidal anthranilamides

This invention provides a composition comprising a first compound selected from Formula 1, an N-oxide or an agriculturally suitable salt thereof; and a second compound selected from insecticidal macrocyclic lactones, wherein R 1 , R 2 , R 3 , R 4a , R 4b and R 5 are as defined in the disclosure.

Arthropodicidal anthranilamides

This invention provides a composition comprising a first compound selected from Formula 1, an N-oxide or an agriculturally suitable salt thereof; and a second compound selected from neonicotinoids, wherein R 1 , R 2 , R 3 , R 4a , R 4b and R 5 are as defined in the disclosure.

Arthropodicidal anthranilamides

This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R 1 , R 2 , R 3 , R 4a , R 4b and R 5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.

Arthropodicidal anthranilamides

This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R 1 , R 2 , R 3 , R 4a , R 4b and R 5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.

Anthropodicidal anthranilamides

This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R 1 , R 2 , R 3 , R 4a , R 4b and R 5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.

Synthesis of substituted pyrazoline carboxamidine derivatives

FIELD: chemistry. SUBSTANCE: invention relates to a method of producing pyrazoline carboxamidine derivatives of formula . Said compounds are known as powerful 5-HT 6 antagonists. The disclosed method comprises reacting a corresponding substituted 4,5-dihydro-(1H)-pyrazole or an isomer thereof with isothiocyanate R 6 -N=C=S to obtain an amide of substituted 4,5-dihydro-(1H)-pyrazole-1-carbothioic acid or tautomeric substituted 4,5-dihydro-(1H)-pyrazole-1-carboxymidothioic acid . The obtained intermediate compounds are reacted with a corresponding alkylating agent to obtain an intermediate S-alkylated compound . Said intermediate compound is reacted with a sulphonamide derivative R 7 SO 2 NH 2 and the target compound of formula (I) is separated from the reaction mixture. The invention also relates to novel intermediate products (III a ), (III b ) and (IV). Symbols given in the formulae have values given in the description. EFFECT: providing an alternative method which improves atom efficiency of synthesis of desired compounds with higher output compared to existing methods for synthesis of said compounds. 8 cl, 1 tbl, 3 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 231/06 C07D 231/54 C07D 403/12 C07D 409/04 C07D 409/12 C07D 491/107 (13) 2 550 694 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2012136831/04, 27.01.2011 (24) Дата начала отсчета срока действия патента: 27.01.2011 Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы): ВАН ЛУВЕЗЕЙН Арнольд (NL), ЛАНГЕ Йозефус Х. М. (NL), БАРФ Геррит А. (NL), ДЕН ХАРТОГ Арнольд П. (NL) R U (73) Патентообладатель(и): ЭББВИ БАХАМАЗ ЛТД. (BS) 29.01.2010 US 61/299,363; 29.01.2010 EP 10152097.1 (43) Дата публикации заявки: 10.03.2014 Бюл. № 7 2 5 5 0 6 9 4 (45) Опубликовано: 10.05.2015 Бюл. № 13 (56) Список документов, цитированных в отчете о поиске: WO2009/115515 A1, 24.09.2009; . ЕА 2009703310 А1, ...

Hydrazide compound and use of the same in pest control

There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitro-gen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.

Method for controlling particular insect pests by applying anthranilamide compounds

Heterocyclic substituted-amino-pyrazolines

This invention relates to novel 3-amino-1-heteroaryl-2-pyrazolines and their C 4 and C 5 analogs, useful for meliorating the inflammation and/or the progressive joint deterioration characteristic of arthritic disease, preventing the onset of asthmatic symptoms and allergic diseases, or as analgesic, antibacterial or antifungal agents.

Patent FR2068471B1

PHENYLCARBAMOYL-PYRAZOLINES, PROCESS FOR THEIR PREPARATION AND THE USE OF SUCH COMPOUNDS AS INSECTICIDES

Colour stable bactericidal soap

Clear coloured fatty acid alkaline soaps, contng. one of hydrazine, hydroxylamine, and alkaline salts of (S2 and 4 valent) sulphoxo acids pref. 0.01-5 wt.% as reducing agent, also contain (a) 0.001-1 wt.% optical brightener of formula: where X is alkaline metal, and (b) 0.1-5 wt.% of 2-hydroxy-2',4,4'-trichlorodiphenyl ether. Pref. up to 2 wt.% of amino polycarboxylates esp. alkaline metal-EDTA and/or polyphosphonates esp. alkali metal-amino tris(methylenephosphonate) are included as complexing agents.

Optical brighteners

Patent FR2106632B1

Patent FR2262662B1

NEW PHENYLCARBAMOYL-2-PYRAZOLINES SUBSTITUTES, THEIR METHOD OF PREPARATION AND THEIR APPLICATION AS INSECTICIDES

L'invention concerne des phénylcarbamoyl-2-pyrazolines substituées. On obtient ces composés par un procédé qui consiste à faire réagir des 2-pyrazolines avec des isocyanates de phényle en présence éventuelle d'un solvant. Les composés de l'invention sont doués d'une bonne activité insecticide. The invention relates to substituted phenylcarbamoyl-2-pyrazolines. These compounds are obtained by a process which consists in reacting 2-pyrazolines with phenyl isocyanates in the optional presence of a solvent. The compounds of the invention are endowed with good insecticidal activity.

DITHIOACYLDIHYDROPYRAZOLE CARBOXYLIC ACID DERIVATIVES, DITHIOACYLPROLINE DERIVATIVES, AND RELATED COMPOUNDS WITH ANTIHYPERTENSIVE ACTION

COMPOSE AYANT POUR FORMULE: (CF DESSIN DANS BOPI) OU: (CF DESSIN DANS BOPI) AINSI QUE SES SELS BASIQUES, FORMULES DANS LESQUELLES: R EST UN ATOME D'HYDROGENE OU UN RADICAL ALKYLE, ARYLE OU ARYLALKYLE; R EST UN ATOME D'HYDROGENE ET R EST UN ATOME D'HYDROGENE OU D'HALOGENE OU UN GROUPEMENT HYDROXY OU ALCOXY, OU BIEN R ET R FORMENT ENSEMBLE O OU -X-(CH)-X- OU X EST UN ATOME D'OXYGENE OU DE SOUFRE, ET T EST EGAL A 2 OU 3; R EST UN ATOME D'HYDROGENE OU UN RADICAL ALKYLE; R EST UN ATOME D'HYDROGENE OU UN RADICAL ALKYLE OU TRIFLUOROMETHYLE; R EST UN RADICAL ALKYLE AYANT DE 1 A 20ATOMES DE CARBONE, UN RADICAL ARYLE OU ARYLALKYLE OU UN GROUPEMENT HETEROCYCLIQUE A 5 OU 6CHAINONS DONT LE CYCLE COMPORTE UN OU DEUX ATOMES D'AZOTE, D'OXYGENE OU DE SOUFRE; R EST UN RADICAL ARYLE; M EST EGAL A 0, 1 OU 2; ET N EST EGAL A 1 OU 2. CES COMPOSES ONT UNE ACTION ANTIHYPERTENSIVE. COMPOUND HAS THE FORMULA: (CF DRAWING IN BOPI) OR: (CF DRAWING IN BOPI) AS WELL AS ITS BASIC SALTS, FORMULAS IN WHICH: R IS AN ATOM OF HYDROGEN OR A RADICAL ALKYL, ARYL OR ARYLALKYL; R IS A HYDROGEN ATOM AND R IS A HYDROGEN OR HALOGEN ATOM OR A HYDROXY OR ALCOXY GROUP, OR R AND R FORM TOGETHER O OR -X- (CH) -X- OR X IS AN ATOM D 'OXYGEN OR SULFUR, AND T IS 2 OR 3; R IS A HYDROGEN ATOM OR A RADICAL ALKYL; R IS A HYDROGEN ATOM OR A RADICAL ALKYL OR TRIFLUOROMETHYL; R IS A RADICAL ALKYL WITH 1 TO 20 ATOMS OF CARBON, AN ARYL OR ARYLALKYL RADICAL OR A 5 OR 6 CHAIN HETEROCYCLIC GROUP WHOSE CYCLE CONTAINS ONE OR TWO ATOMS OF NITROGEN, OXYGEN OR SULFUR; R IS A RADICAL ARYL; M IS EQUAL TO 0, 1 OR 2; AND N IS EQUAL TO 1 OR 2. THESE COMPOUNDS HAVE ANTIHYPERTENSIVE ACTION.